Paperbase

Vincent Delorme

Delorme Vincent

ORCID: 0000-0001-5235-7069

Discovery of thienothiazolocarboxamide analogues as novel anti-tubercular agent. 10.1016/j.bmc.2020.115797

Drug Discovery Platform Targeting M. tuberculosis with Human Embryonic Stem Cell-Derived Macrophages. 10.1016/j.stemcr.2019.10.002

Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis. 10.1016/j.bioorg.2018.08.025

Molecular Targets Related Drug Resistance Mechanisms in MDR-, XDR-, and TDR-Mycobacterium tuberculosis Strains. 10.3389/fcimb.2018.00114

Publisher Correction: Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles. 10.1038/s41598-018-25177-2

Mycobacterium tuberculosis Infection and Innate Responses in a New Model of Lung Alveolar Macrophages. 10.3389/fimmu.2018.00438

ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton. 10.15252/embr.201744371

Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis. 10.1038/s41598-017-11843-4

Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling. 10.1016/j.celrep.2017.08.101

Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles. 10.1038/s41598-017-05453-3

Efflux Attenuates the Antibacterial Activity of Q203 in Mycobacterium tuberculosis. 10.1128/aac.02637-16

Phenotypic assays for Mycobacterium tuberculosis infection. 10.1002/cyto.a.23129

Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays. 10.1021/acschembio.7b00091

Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420. 10.1126/science.aag1006

High-Content Screening of Raw Actinomycete Extracts for the Identification of Antituberculosis Activities. 10.1177/1087057116675887

Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria. 10.1111/mmi.13535

STAT3 Represses Nitric Oxide Synthesis in Human Macrophages upon Mycobacterium tuberculosis Infection. 10.1038/srep29297

A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters. 10.1039/c5ob02630j

Testing chemical and genetic Modulators in Mycobacterium tuberculosis infected cells using phenotypic assays. 10.1007/978-1-4939-2450-9_24

2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1. 10.1021/cb5007163

Supported inhibitor for fishing lipases in complex biological media and mass spectrometry identification. 10.1016/j.biochi.2014.07.015

A microscopic phenotypic assay for the quantification of intracellular mycobacteria adapted for high-throughput/high-content screening. 10.3791/51114

Analysis of the discriminative inhibition of mammalian digestive lipases by 3-phenyl substituted 1,3,4-oxadiazol-2(3H)-ones. 10.1016/j.ejmech.2012.10.040

MmPPOX inhibits Mycobacterium tuberculosis lipolytic enzymes belonging to the hormone-sensitive lipase family and alters mycobacterial growth. 10.1371/journal.pone.0046493

Inhibition of phospholipase A1, lipase and galactolipase activities of pancreatic lipase-related protein 2 by methyl arachidonyl fluorophosphonate (MAFP). 10.1016/j.bbalip.2012.07.014

Effects of surfactants on lipase structure, activity, and inhibition. 10.1007/s11095-010-0362-9

CO2 binding by dynamic combinatorial chemistry: an environmental selection. 10.1021/ja909975q

Two cutinase-like proteins secreted by Mycobacterium tuberculosis show very different lipolytic activities reflecting their physiological function. 10.1096/fj.09-144766

Synthesis and kinetic evaluation of cyclophostin and cyclipostins phosphonate analogs as selective and potent inhibitors of microbial lipases. 10.1021/jm301216x

Phenotypic Screening for Drug Discovery in Tuberculosis https://doi.org/10.1039/9781839160721-00198

Giovanna RICCARDI

RICCARDI Giovanna

ORCID: 0000-0003-3295-0070

Mycobacterium tuberculosis: Drug resistance and future perspectives 10.2217/fmb.09.20

Sequence of the Bacillus stearothermophilus gene encoding aspartokinase II 10.1016/0378-1119(95)00834-9

Antituberculars which target decaprenylphosphoryl-β-Dribofuranose 2′-oxidase DprE1: State of art 10.1007/s00253-012-4013-4

Gene arrangement and organization in a ~ 76 kb fragment: Encompassing the oriC region of the chromosome of Mycobacterium leprae 10.1099/13500872-142-11-3147

Organization of the origins of replication of the chromosomes of Mycobacterium smegmatis, Mycobacterium leprae and Mycobacterium tuberculosis and isolation of a functional origin from M. smegmatis 10.1111/j.1365-2958.1996.tb02617.x

Detection and characterization of naturally occurring plasmids in Bacillus licheniformis 10.1111/j.1574-6968.1991.tb04781.x

Molecular mechanisms of chlorhexidine tolerance in Burkholderia cenocepacia biofilms 10.1128/AAC.01571-10

Differential roles of rnd efflux pumps in antimicrobial drug resistance of sessile and planktonic burkholderia cenocepacia cells 10.1128/AAC.03800-14

Erratum: Antituberculars which target decaprenylphosphoryl-β-D- ribofuranose 2'-oxidase DprE1: State of art (Applied Microbiology and Biotechnology (2012) 94 (907-916) DOI: 10.1007/s00253-012-4013-4) 10.1007/s00253-012-4217-7

Antibiotic resistance of benthic bacteria in fish-farm and control sediments of the Western Mediterranean 10.1016/S0044-8486(03)00016-4

Amino acid biosynthesis and its regulation in cyanobacteria 10.1016/0168-9452(89)90018-6

Characterization of Gram-positive broad host-range plasmids carrying a thermophilic replicon 10.1016/0923-2508(91)90108-M

4-Aminoquinolone piperidine amides: Noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity 10.1021/jm5005978

Evaluation of fluoroquinolone resistance mechanisms in Pseudomonas aeruginosa multidrug resistance clinical isolates 10.1089/mdr.2011.0019

Benzothiazinones Kill Mycobacterium tuberculosis by blocking Arabinan synthesis 10.1126/science.1171583

Assessment of three Resistance-Nodulation-Cell Division drug efflux transporters of Burkholderia cenocepacia in intrinsic antibiotic resistance 10.1186/1471-2180-9-200

Erratum: Global analysis of the Mycobacterium tuberculosis zur (FurB) regulon (Journal of Bacteriology (2007) 189, 3, (730-740)) 10.1128/JB.00593-07

Molecular characterization of the genes encoding acetohydroxy acid synthase in the cyanobacterium Spirulina platensis 10.1099/00221287-138-7-1399

Efflux pump genes of the resistance-nodulation-division family in Burkholderia cenocepacia genome 10.1186/1471-2180-6-66

Role of mycobacterial efflux transporters in drug resistance: An unresolved question 10.1111/j.1574-6976.2005.00002.x

Phenotypic and Genotypic Characterisation of Burkholderia cenocepacia J2315 Mutants Affected in Homoserine Lactone and Diffusible Signal Factor-Based Quorum Sensing Systems Suggests Interplay between Both Types of Systems 10.1371/journal.pone.0055112

Molecular approaches to pathogenesis study of Burkholderia cenocepacia, an important cystic fibrosis opportunistic bacterium 10.1007/s00253-011-3616-5

Heterologous expression, purification, and enzymatic activity of Mycobacterium tuberculosis NAD⁺ synthetase 10.1016/S1046-5928(02)00041-4

Transcriptional analysis of ESAT-6 cluster 3 in Mycobacterium smegmatis 10.1186/1471-2180-9-48

Genomic analysis of zinc homeostasis in Mycobacterium tuberculosis 10.1111/j.1574-6968.2008.01320.x

Mechanism of resistance to an antitubercular 2-thiopyridine derivative that is also active against Burkholderia cenocepacia 10.1128/AAC.02438-13

Determination of a 15437 bp nucleotide sequence around the inhA gene of Mycobacterium avium and similarity analysis of the products of putative ORFs 10.1099/00221287-144-3-807

Biochemical evidence for multiple forms of acetohydroxy acid synthase in Spirulina platensis 10.1007/BF00252216

Investigating the mechanism of action of diketopiperazines inhibitors of the burkholderia cenocepacia quorum sensing synthase CepI: A site-directed mutagenesis study 10.3389/fphar.2018.00836

Structural basis for benzothiazinone-mediated killing of Mycobacterium tuberculosis 10.1126/scitranslmed.3004395

Biochemical characterization of glutamate Racemase - A new candidate drug target against Burkholderia cenocepacia infections 10.1371/journal.pone.0167350

Cloning and sequencing of the ilvBNC gene cluster from Mycobacterium avium 10.1016/0378-1119(96)00275-2

Rv2466c mediates the activation of TP053 to kill replicating and non-replicating Mycobacterium tuberculosis 10.1021/cb500149m

Azole resistance in Mycobacterium tuberculosis is mediated by the MmpS5-MmpL5 efflux system 10.1016/j.tube.2008.08.003

Molecular cloning and expression of Spirulina platensis acetohydroxy acid synthase genes in Escherichia coli 10.1007/BF00243456

Development of a repressible mycobacterial promoter system based on two transcriptional repressors 10.1093/nar/gkq235

Characterisation and antimicrobial activity of epibiotic bacteria from Petrosia ficiformis (Porifera, Demospongiae) 10.1016/j.jembe.2004.03.006

Genetic transformation of intact cells of Bacillus subtilis by electroporation 10.1016/0378-1097(90)90182-P

Transcriptional regulation of furA and katG upon oxidative stress in Mycobacterium smegmatis 10.1128/JB.183.23.6801-6806.2001

Mechanism of action of 5-nitrothiophenes against mycobacterium tuberculosis 10.1128/AAC.02693-13

The DprE1 enzyme, one of the most vulnerable targets of Mycobacterium tuberculosis 10.1007/s00253-013-5218-x

Burkholderia cenocepacia infections in cystic fibrosis patients: Drug resistance and therapeutic approaches 10.3389/fmicb.2017.01592

Structural organization of pBC1, a cryptic plasmid from Bacillus coagulans 10.1128/jb.174.2.638-642.1992

Vaccines to Overcome Antibiotic Resistance: The Challenge of Burkholderia cenocepacia 10.1016/j.tim.2019.12.005

Raising awareness of the importance of funding for tuberculosis small-molecule research 10.1016/j.drudis.2016.09.012

Bacterial community structure and activity in fish farm sediments of the Ligurian Sea (Western Mediterranean) 10.1023/A:1021365829687

Biological and structural characterization of the Mycobacterium smegmatis nitroreductase NfnB, and its role in benzothiazinone resistance 10.1111/j.1365-2958.2010.07277.x

The Crystal Structure of Burkholderia cenocepacia DfsA Provides Insights into Substrate Recognition and Quorum Sensing Fatty Acid Biosynthesis 10.1021/acs.biochem.6b00178

The cell division protein FtsZ as a cellular target to hit cystic fibrosis pathogens 10.1016/j.ejmech.2020.112132

A Phenotypic Based Target Screening Approach Delivers New Antitubercular CTP Synthetase Inhibitors 10.1021/acsinfecdis.7b00006

Deciphering the role of rnd efflux transporters in burkholderia cenocepacia 10.1371/journal.pone.0018902

Exploring the HME and HAE1 efflux systems in the genus Burkholderia 10.1186/1471-2148-10-164

Plasmid screening in thermophilic Bacillus: Physical characterization and molecular cloning 10.1007/BF01568897

The Mycobacterium tuberculosis Rv2358-furB operon is induced by zinc 10.1016/j.resmic.2003.11.009

New prodrugs against tuberculosis 10.1016/j.drudis.2016.09.006

Decaprenylphosphoryl-β-D-ribose 2'-epimerase from Mycobacterium tuberculosis is a magic drug target 10.2174/092986710791959693

Molecular cloning and sequencing of the β-isopropylmalate dehydrogenase gene from the cyanobacterium Spirulina platensis 10.1099/00221287-138-3-493

Cloning of the glutamine synthetase gene from spirulina platensis 10.1007/BF02418760

Characterization of a mutant of chlamydomonas reinhardtII resistant to fusidic acid 10.1016/0014-5793(81)81166-0

Discovery of new diketopiperazines inhibiting Burkholderia cenocepacia quorum sensing in vitro and in vivo 10.1038/srep32487

A highly efficient electroporation system for transformation of Bacillus licheniformis 10.1007/BF00152745

Competitive fitness of essential gene knockdowns reveals a broad-spectrum antibacterial inhibitor of the cell division protein FtsZ 10.1128/AAC.01231-18

A census of RND superfamily proteins in the Burkholderia genus 10.2217/fmb.13.50

LfrR is a repressor that regulates expression of the efflux pump LfrA in Mycobacterium smegmatis 10.1128/AAC.00656-06

Global analysis of the Mycobacterium tuberculosis Zur (FurB) regulon 10.1128/JB.01190-06

Mycobacterium tuberculosis phosphoribosylpyrophosphate synthetase: Biochemical features of a crucial enzyme for mycobacterial cell wall biosynthesis 10.1371/journal.pone.0015494

New tuberculosis drugs on the horizon 10.1016/j.mib.2011.07.022

A multitarget approach to drug discovery inhibiting Mycobacterium tuberculosis PyrG and PanK 10.1038/s41598-018-21614-4

Rv2358 and FurB: Two transcriptional regulators from Mycobacterium tuberculosis which respond to zinc 10.1128/JB.187.16.5837-5840.2005

Mycobacterium tuberculosis H37Rv comparative gene-expression analysis in synthetic medium and human macrophage 10.1016/S0378-1119(00)00249-3

In vitro translation of chloroplast mRNAs 10.1016/0304-4211(82)90148-1

High content screening identifies decaprenyl-phosphoribose 2′ epimerase as a target for intracellular antimycobacterial inhibitors 10.1371/journal.ppat.1000645

The redox state regulates the conformation of Rv2466c to activate the antitubercular prodrug TP053 10.1074/jbc.M115.677039

Biofilm-Grown Burkholderia cepacia Complex Cells Survive Antibiotic Treatment by Avoiding Production of Reactive Oxygen Species 10.1371/journal.pone.0058943

Identification and characterization of a new ligand-binding site in FnbB, a fibronectin-binding adhesin from Streptococcus dysgalactiae 10.1016/S1570-9639(03)00020-7

Analogous mechanisms of resistance to benzothiazinones and dinitrobenzamides in Mycobacterium smegmatis 10.1371/journal.pone.0026675

Erratum: Rv2358 and FurB: Two transcriptional regulators from Mycobacterium tuberculosis which respond to zinc (Journal of Bacteriology (2005) 187, 16 (5837-5840)) 10.1128/JB.00141-07

Glutamine amidotransferase activity of NAD⁺ synthetase from Mycobacterium tuberculosis depends on an amino-terminal nitrilase domain 10.1016/j.resmic.2004.08.011

Techniques and Applications: The heterologous expression of Mycobacterium tuberculosis genes is an uphill road 10.1016/S0966-842X(03)00180-X

Characterization of mutants of Spirulina platensis resistant to amino acid analogues 10.1111/j.1574-6968.1981.tb07668.x

The TB structural genomics consortium: A resource for Mycobacterium tuberculosis biology 10.1016/S1472-9792(03)00051-9

Clinical isolates of Mycobacterium tuberculosis in four European hospitals are uniformly susceptible to benzothiazinones 10.1128/AAC.01676-09

New shuttle vector for cloning in Bacillus stearothermophilus 10.1016/0923-2508(94)90074-4

Biochemical characterization and cloning of acetohydroxy acid synthase from spirulina platensis 10.1080/11263509009430656

Structural plasticity and distinct drug-binding modes of LfrR, a mycobacterial efflux pump regulator 10.1128/JB.00631-09

Trends in discovery of new drugs for tuberculosis therapy 10.1038/ja.2014.109

DprE1, a new taxonomic marker in mycobacteria 10.1111/1574-6968.12246

Efflux-mediated resistance to a benzothiadiazol derivative effective against Burkholderia cenocepacia 10.3389/fmicb.2015.00815

mmpL7 gene of Mycobacterium tuberculosis is responsible for isoniazid efflux in Mycobacterium smegmatis 10.1128/AAC.49.11.4775-4777.2005

Rv2686c-Rv2687c-Rv2688c, an ABC fluoroquinolone efflux pump in Mycobacterium tuberculosis 10.1128/AAC.48.8.3175-3178.2004

Contribution of the multidrug efflux pump LfrA to innate mycobacterial drug resistance 10.1016/S0378-1097(00)00456-0

Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG 10.1016/j.chembiol.2015.05.016

Mycobacterium tuberculosis fura autoregulates its own expression 10.1128/JB.185.18.5357-5362.2003

PEGylated mucus-penetrating nanocrystals for lung delivery of a new FtsZ inhibitor against Burkholderia cenocepacia infection 10.1016/j.nano.2019.102113

Benzothiazinones are suicide inhibitors of mycobacterial decaprenylphosphoryl-β-d-ribofuranose 2′-oxidase DprE1 10.1021/ja211042r

New Insights into the Mechanism of Action of the Thienopyrimidine Antitubercular Prodrug TP053 10.1021/acsinfecdis.9b00388

2-carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1 10.1021/cb5007163

The katE gene, which encodes the catalase HPII of Mycobacterium avium 10.1046/j.1365-2958.1996.352876.x

Sequence of the gene encoding an alkaline serine protease of thermophilic Bacillus smithii 10.1016/0378-1119(94)90340-9

Cloning, sequencing and expression of the ilvBNC gene cluster from Streptomyces avermitilis 10.1016/0378-1119(95)00563-4

Neeraj Dhar

Dhar Neeraj

ORCID: 0000-0002-5887-8137

Dynamic Persistence of Antibiotic-Stressed Mycobacteria 10.1126/science.1229858

Mycobacterium tuberculosisEspB binds phospholipids and mediates EsxA-independent virulence 10.1111/mmi.12336

Single-cell dynamics of the chromosome replication and cell division cycles in mycobacteria 10.1038/ncomms3470

EspD Is Critical for the Virulence-Mediating ESX-1 Secretion System in Mycobacterium tuberculosis 10.1128/JB.06417-11

Malachite Green Interferes with Postantibiotic Recovery of Mycobacteria 10.1128/AAC.00406-12

Streptomycin-Starved Mycobacterium tuberculosis 18b, a Drug Discovery Tool for Latent Tuberculosis 10.1128/AAC.01125-12

Structural Basis for Benzothiazinone-Mediated Killing of Mycobacterium tuberculosis 10.1126/scitranslmed.3004395

Nanoparticle conjugation and pulmonary delivery enhance the protective efficacy of Ag85B and CpG against tuberculosis 10.1016/j.vaccine.2011.07.039

Development of a repressible mycobacterial promoter system based on two transcriptional repressors 10.1093/nar/gkq235

Mycobacterium tuberculosis persistence mutants identified by screening in isoniazid-treated mice 10.1073/pnas.1003219107

Simple Model for Testing Drugs against Nonreplicating Mycobacterium tuberculosis 10.1128/AAC.00821-10

Benzothiazinones Kill Mycobacterium tuberculosis by Blocking Arabinan Synthesis 10.1126/science.1171583

Boosting with a DNA vaccine expressing ESAT-6 (DNAE6) obliterates the protection imparted by recombinant BCG (rBCGE6) against aerosol Mycobacterium tuberculosis infection in guinea pigs 10.1016/j.vaccine.2009.09.121

Enhanced and Enduring Protection against Tuberculosis by Recombinant BCG-Ag85C and Its Association with Modulation of Cytokine Profile in Lung 10.1371/journal.pone.0003869

Microbial phenotypic heterogeneity and antibiotic tolerance 10.1016/j.mib.2006.12.007

Elicitation of efficient, protective immune responses by using DNA vaccines against tuberculosis 10.1016/j.vaccine.2005.03.056

Increased expression of Mycobacterium tuberculosis 19 kDa lipoprotein obliterates the protective efficacy of BCG by polarizing host immune responses to the Th2 subtype 10.1111/j.1365-3083.2005.01569.x

Immunogenicity of recombinant BCG vaccine strains overexpressing components of the antigen 85 complex of Mycobacterium tuberculosis 10.1007/s00430-002-0170-x

Disruption of mptpB impairs the ability of Mycobacterium tuberculosis to survive in guinea pigs 10.1046/j.1365-2958.2003.03712.x

Modulation of host immune responses by overexpression of immunodominant antigens of Mycobacterium tuberculosis in bacille Calmette-Guerin 10.1046/j.1365-3083.2003.01321.x

Skewing of the Th1/Th2 responses in mice due to variation in the level of expression of an antigen in a recombinant BCG system 10.1016/S0165-2478(03)00043-9

4-Aminoquinolone Piperidine Amides: Noncovalent Inhibitors of DprE1 with Long Residence Time and Potent Antimycobacterial Activity 10.1021/jm5005978

Assessing the essentiality of the decaprenyl-phospho-D-arabinofuranose pathway in Mycobacterium tuberculosis using conditional mutants 10.1111/mmi.12546

Delayed bactericidal response of Mycobacterium tuberculosis to bedaquiline involves remodelling of bacterial metabolism 10.1038/ncomms4369

Dielectrophoresis-based purification of antibiotic-treated bacterial subpopulations 10.1039/c4lc00109e

In Vitro and In Vivo Activities of Three Oxazolidinones against Nonreplicating Mycobacterium tuberculosis 10.1128/AAC.02410-14

Phenotypic Profiling of Mycobacterium tuberculosis EspA Point Mutants Reveals that Blockage of ESAT-6 and CFP-10 Secretion In Vitro Does Not Always Correlate with Attenuation of Virulence 10.1128/JB.00967-13

Bioluminescence for assessing drug potency against nonreplicating Mycobacterium tuberculosis 10.1128/AAC.00528-15

2-carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1 10.1021/cb5007163

Rapid cytolysis of mycobacterium tuberculosis by faropenem, an orally bioavailable β-lactam antibiotic 10.1128/AAC.03461

Stressed mycobacteria use the chaperone ClpB to sequester irreversibly oxidized proteins asymmetrically within and between cells 10.1016/j.chom.2014.12.008

Stress and host immunity amplify mycobacterium tuberculosis phenotypic heterogeneity and induce nongrowing metabolically active forms 10.1016/j.chom.2014.11.016

Single-cell analysis of mycobacteria using microfluidics and time-lapse microscopy 10.1007/978-1-4939-2450-9_14

Simple and rapid method to determine antimycobacterial potency of compounds by using autoluminescent mycobacterium tuberculosis 10.1128/AAC.03205-14

The phosphatidyl-myo-inositol mannosyltransferase PimA is essential for Mycobacterium tuberculosis growth in vitro and in vivo 10.1128/JB.01346-13

EspI regulates the ESX-1 secretion system in response to ATP levels in Mycobacterium tuberculosis 10.1111/mmi.12718

Recombinant BCG approach for development of vaccines: Cloning and expression of immunodominant antigens of M. tuberculosis 10.1016/S0378-1097(00)00353-0

Whole Cell Target Engagement Identifies Novel Inhibitors of Mycobacterium tuberculosis Decaprenylphosphoryl-β- d -ribose Oxidase 10.1021/acsinfecdis.5b00065

Combinations of β-lactam antibiotics currently in clinical trials are efficacious in a dhp-i-deficient mouse model of tuberculosis infection 10.1128/AAC.01063-15

Rapid cytolysis of Mycobacterium tuberculosis by faropenem, an orally bioavailable β-lactam antibiotic 10.1128/AAC.03461-14

Erratum to The Phosphatidyl-myo-Inositol Mannosyltransferase PimA Is Essential for Mycobacterium tuberculosis Growth In Vitro and In Vivo [Journal of Bacteriology, 196, 19, (2014) 3441-3451] DOI: 10.1128/JB.02332-14 10.1128/JB.02332-14

Antitubercular drugs for an old target: GSK693 as a promising InhA direct inhibitor 10.1016/j.ebiom.2016.05.006

Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria 10.1111/mmi.13535

An Amidase_3 domain-containing N-acetylmuramyl-L-alanine amidase is required for mycobacterial cell division 10.1038/s41598-017-01184-7

Division site selection linked to inherited cell surface wave troughs in mycobacteria 10.1038/nmicrobiol.2017.94

Elucidating the role of (p)ppGpp in mycobacterial persistence against antibiotics 10.1002/iub.1888

Preexisting variation in DNA damage response predicts the fate of single mycobacteria under stress 10.15252/embj.2019101876

Computational Analysis of the Mutual Constraints between Single‐Cell Growth and Division Control Models 10.1002/adbi.201900103

A lung-on-chip model reveals an essential role for alveolar epithelial cells in controlling bacterial growth during early tuberculosis 10.1101/2020.02.03.931170

Driving polar growth 10.7554/eLife.57043

Dielectrophoresis as a single cell characterization method for bacteria 10.1088/2057-1976/3/1/015005

Early invasion of uropathogenic Escherichia coli into the bladder wall by solitary bacteria that are protected from antibiotics and neutrophil swarms in an organoid model 10.1101/2020.10.29.358622

A lung-on-chip model of early Mycobacterium tuberculosis infection reveals an essential role for alveolar epithelial cells in controlling bacterial growth 10.7554/eLife.59961

Dynamic persistence of intracellular bacterial communities of uropathogenic Escherichia coli in a human bladder-chip model of urinary tract infections 10.1101/2021.01.03.424836

Rapid endotheliitis and vascular damage characterize SARS‐CoV‐2 infection in a human lung‐on‐chip model 10.15252/embr.202152744

Dynamic persistence of UPEC intracellular bacterial communities in a human bladder-chip model of urinary tract infection 10.7554/eLife.66481

Early invasion of the bladder wall by solitary bacteria protects UPEC from antibiotics and neutrophil swarms in an organoid model 10.1016/j.celrep.2021.109351

Rosaria Luciani

Luciani Rosaria

ORCID: 0000-0003-1367-0217

Discovery of highly potent acid ceramidase inhibitors with in vitro tumor chemosensitizing activity 10.1038/srep01035

Collateral sensitivity to novel thymidylate synthase inhibitors correlates with folate cycle enzymes impairment in cisplatin-resistant human ovarian cancer cells 10.1016/j.ejphar.2009.04.062

Ligand-based virtual screening and ADME-tox guided approach to identify triazolo-quinoxalines as folate cycle inhibitors 10.1016/j.bmc.2010.09.065

2′-Deoxyuridine 5′-Monophosphate Substrate Displacement in Thymidylate Synthase through 6-Hydroxy-2 H -naphtho[1,8- bc ]furan-2-one Derivatives 10.1021/jm4014086

Virtual Screening Identification of Nonfolate Compounds, Including a CNS Drug, as Antiparasitic Agents Inhibiting Pteridine Reductase 10.1021/jm1010572

Inhibitor of Ovarian Cancer Cells Growth by Virtual Screening: A New Thiazole Derivative Targeting Human Thymidylate Synthase 10.1021/jm300850v

Structure-Based Selectivity Optimization of Piperidine–Pteridine Derivatives as Potent Leishmania Pteridine Reductase Inhibitors 10.1021/jm300563f

2-[N-Alkyl(R-phenyl)-aminomethyl]-3-phenyl-7-trifluoromethylquinoxalines as anticancer agents inhibitors of folate enzymes 10.1016/j.ejmech.2014.01.048

Identification of the Binding Modes of N -Phenylphthalimides Inhibiting Bacterial Thymidylate Synthase through X-Ray Crystallography Screening 10.1021/jm2005018

Optimization of Peptides That Target Human Thymidylate Synthase to Inhibit Ovarian Cancer Cell Growth 10.1021/jm401574p

The structure of Enterococcus faecalis thymidylate synthase provides clues about folate bacterial metabolism 10.1107/s0907444912026236

2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1 10.1021/cb5007163

Priscille Brodin

Brodin Priscille

ORCID: 0000-0003-0991-7344

Email: priscille.brodin@inserm.fr

How can nanoparticles contribute to antituberculosis therapy? 10.1016/j.drudis.2017.01.011

Host-directed therapies offer novel opportunities for the fight against tuberculosis 10.1016/j.drudis.2017.05.005

A Bacterial Toxin with Analgesic Properties: Hyperpolarization of DRG Neurons by Mycolactone 10.3390/toxins9070227

A Bacterial Toxin with Analgesic Properties: Hyperpolarization of DRG Neurons by Mycolactone 10.3390/toxins9070227 10.3390/toxins9070227.

Clofazimine encapsulation in nanoporous silica particles for the oral treatment of antibiotic-resistant Mycobacterium tuberculosis infections 10.2217/nnm-2016-0364

Cyclodextrin-based nanocarriers containing a synergic drug combination: a potential formulation for pulmonary administration of antitubercular drugs 10.1016/j.ijpharm.2017.05.030 10.1016/j.ijpharm.2017.05.030.

Genome-wide, high-content siRNA screening identifies the Alzheimer's genetic risk factor FERMT2 as a major modulator of APP metabolism 10.1007/s00401-016-1652-z

Host-directed therapies offer novel opportunities for the fight against tuberculosis 10.1016/j.drudis.2017.05.005 10.1016/j.drudis.2017.05.005.

Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria 10.1111/mmi.13535

Impact of pe_ pgrs33 Gene Polymorphisms on Mycobacterium tuberculosis Infection and Pathogenesis 10.3389/fcimb.2017.00137

LppM impact on the colonization of macrophages by Mycobacterium tuberculosis 10.1111/cmi.12619

Phenotypic assays for Mycobacterium tuberculosis infection 10.1002/cyto.a.23129 10.1002/cyto.a.23129.

Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420 10.1126/science.aag1006

A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters 10.1039/c5ob02630j

Khaya grandifoliola C.DC: a potential source of active ingredients against hepatitis C virus in vitro 10.1007/s00705-016-2771-5

Mycobacterium tuberculosis LppM Displays an Original Structure and Domain Composition Linked to a Dual Localization 10.1016/j.str.2016.07.009

Mycolactone The amazing analgesic mycobacterial toxin 10.1051/medsci/20163202007

STAT3 Represses Nitric Oxide Synthesis in Human Macrophages upon Mycobacterium tuberculosis Infection 10.1038/srep29297

2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1 10.1021/cb5007163

Cytosolic Access of Mycobacterium tuberculosis: Critical Impact of Phagosomal Acidification Control and Demonstration of Occurrence In Vivo 10.1371/journal.ppat.1004650

High content screening in chemical biology: overview and main challenges 10.1051/medsci/20153102016

High-Content Screening Technology Combined with a Human Granuloma Model as a New Approach To Evaluate the Activities of Drugs against Mycobacterium tuberculosis 10.1128/aac.03705-14

Increased protective efficacy of recombinant BCG strains expressing virulence-neutral proteins of the ESX-1 secretion system 10.1016/j.vaccine.2015.03.083

Plant extracts from Cameroonian medicinal plants strongly inhibit hepatitis C virus infection in vitro 10.3389/fmicb.2015.00438

Polyphenols Inhibit Hepatitis C Virus Entry by a New Mechanism of Action 10.1128/jvi.01473-15

Testing chemical and genetic Modulators in Mycobacterium tuberculosis infected cells using phenotypic assays 10.1007/978-1-4939-2450-9_24

A Microscopic Phenotypic Assay for the Quantification of Intracellular Mycobacteria Adapted for High-throughput/High-content Screening 10.3791/51114

Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking Approaches 10.1021/jm500422b

Mycobacterial Toxin Induces Analgesia in Buruli Ulcer by Targeting the Angiotensin Pathways 10.1016/j.cell.2014.04.040

Potent antiviral activity of Solanum rantonnetii and the isolated compounds against hepatitis C virus in vitro 10.1016/j.jff.2014.09.022

A novel specific edge effect correction method for RNA interference screenings 10.1093/bioinformatics/btr648

Discovery of Novel N-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis 10.1021/jm3003779

Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200825u

The Balance of Apoptotic and Necrotic Cell Death in Mycobacterium tuberculosis Infected Macrophages Is Not Dependent on Bacterial Virulence 10.1371/journal.pone.0047573

Analogous Mechanisms of Resistance to Benzothiazinones and Dinitrobenzamides in Mycobacterium smegmatis 10.1371/journal.pone.0026675

Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200076a

High-content screening in infectious diseases 10.1016/j.cbpa.2011.05.023

Functional characterization of the Mycobacterium tuberculosis serine/threonine kinase PknJ 10.1099/mic.0.038133-0

High Content Phenotypic Cell-Based Visual Screen Identifies Mycobacterium tuberculosis Acyltrehalose-Containing Glycolipids Involved in Phagosome Remodeling 10.1371/journal.ppat.1001100

High-content imaging of Mycobacterium tuberculosis-infected macrophages: an in vitro model for tuberculosis drug discovery 10.4155/fmc.10.223

Long-circulating DNA lipid nanocapsules as new vector for passive tumor targeting 10.1016/j.biomaterials.2009.09.044

Automated High-Throughput siRNA Transfection in Raw 264.7 Macrophages: A Case Study for Optimization Procedure 10.1177/1087057108328762

Benzothiazinones Kill Mycobacterium tuberculosis by Blocking Arabinan Synthesis 10.1126/science.1171583

High Content Screening Identifies Decaprenyl-Phosphoribose 2 ' Epimerase as a Target for Intracellular Antimycobacterial Inhibitors 10.1371/journal.ppat.1000645

Systematic Genetic Nomenclature for Type VII Secretion Systems 10.1371/journal.ppat.1000507

Control of M-tuberculosis ESAT-6 secretion and specific T cell recognition by PhoP 10.1371/journal.ppat.0040033

Aquatic insects and transmission of Mycobacterium ulcerans 10.1051/medsci/20072367572

ESAT-6 from Mycobacterium tuberculosis dissociates from its putative chaperone CFP-10 under acidic conditions and exhibits membrane-lysing activity 10.1128/jb.00469-07

Impact of Mycobacterium ulcerans biofilm on transmissibility to ecological niches and Buruli ulcer pathogenesis 10.1371/journal.ppat.0030062

Protection against mycobacterium ulcerans lesion development by exposure to aquatic insect saliva 10.1371/journal.pmed.0040064

Support vector machines for automatic detection of tuberculosis bacteria in confocal microscopy images 10.1109/isbi.2007.356794

Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues 10.1016/j.bmc.2006.12.009

An increase in antimycobacterial Th1-cell responses by prime-boost protocols of immunization does not enhance protection against tuberculosis 10.1128/iai.74.4.2128-2137.2006

Benzofuro 3,2-f 1 benzopyrans: A new class of antitubercular agents 10.1016/j.bmc.2006.03.033

Dissection of ESAT-6 system 1 of Mycobacterium tuberculosis and impact on immunogenicity and virulence 10.1128/iai.74.1.88-98.2006

High frequency of CD4(+) T cells specific for the TB10.4 protein correlates with protection against Mycobacterium tuberculosis infection 10.1128/iai.02086-05

Inactivation of Rv2525c, a substrate of the twin arginine translocation (Tat) system of Mycobacterium tuberculosis, increases beta-lactam susceptibility and virulence 10.1128/jb.00631-06

Evaluation of vaccines in the EU TB vaccine cluster using a guinea pig aerosol infection model of tuberculosis 10.1016/j.tube.2004.09.009

Functional analysis of early secreted antigenic target-6, the dominant T-cell antigen of Mycobacterium tuberculosis, reveals key residues involved in secretion, complex formation, virulence, and immunogenicity 10.1074/jbc.M503515200

Immunogenic membrane-associated proteins of Mycobacterium tuberculosis revealed by proteomics 10.1099/mic.0.27799-0

Proteomic identification of M. tuberculosis protein kinase substrates: PknB recruits GarA, a FHA domain-containing protein, through activation loop-mediated interactions 10.1016/j.jmb.2005.05.049

Tuberculosis: from genome to vaccine 10.1586/14760584.4.4.541

Cell envelope protein PPE68 contributes to Mycobacterium tuberculosis RDI immunogenicity independently of a 10-kilodalton culture filtrate protein and ESAT-6 10.1128/iai.72.4.2170-2176.2004

Enhanced protection against tuberculosis by vaccination with recombinant Mycobacterium microti vaccine that induces T cell immunity against region of difference 1 antigens 10.1086/421468

ESAT-6 proteins: protective antigens and virulence factors? 10.1016/j.tim.2004.09.007

Macro-array and bioinformatic analyses reveal mycobacterial 'core' genes, variation in the ESAT-6 gene family and new phylogenetic markers for the Mycobacterium tuberculosis complex 10.1099/mic.0.26662-0

CD8(+)-T-cell responses of mycobacterium-infected mice to a newly identified major histocompatibility complex class I-restricted epitope shared by proteins of the ESAT-6 family 10.1128/iai.71.12.7173-7177.2003

Recombinant BCG exporting ESAT-6 confers enhanced protection against tuberculosis 10.1038/nm859

A new evolutionary scenario for the Mycobacterium tuberculosis complex 10.1073/pnas.052548299

Bacterial artificial chromosome-based comparative genomic analysis identifies Mycobacterium microti as a natural ESAT-6 deletion mutant 10.1128/iai.70.10.5568-5578.2002

Disruption of HIV-1 integrase-DNA complexes by short 6-oxocytosine-containing oligonucleotides 10.1021/bi015732y

Loss of RD1 contributed to the attenuation of the live tuberculosis vaccines Mycobacterium bovis BCG and Mycobacterium microti 10.1046/j.1365-2958.2002.03237.x

6-Oxocytidine containing oligonucleotides inhibit the HIV-1 integrase in vitro 10.1081/ncn-100002322

Determinants of Mg2+-dependent activities of recombinant human immunodeficiency virus type 1 integrase 10.1021/bi000398b

Inhibition of the human immunodeficiency virus type 1 DNA integration by modified oligonucleotides 10.1023/a:1026631910681

Branched oligonucleotide-intercalator conjugate forming a parallel stranded structure inhibits HIV-1 integrase 10.1016/s0014-5793(99)01350-2

Inhibition of HIV-1 integration by mono- & bi-functionalized triple helix forming oligonucleotides 10.1080/07328319908044831

Optimization of alternate-strand triple helix formation at the 5 '-TpA-3 ' and 5 '-ApT-3 ' junctions 10.1093/nar/27.15.3029

A truncated HIV-1 Tat protein basic domain rapidly translocates through the plasma membrane and accumulates in the cell nucleus 10.1074/jbc.272.25.16010

Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids 10.1073/pnas.1707840114

ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton 10.15252/embr.201744371

ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton 10.15252/embr.201744371 10.15252/embr.201744371.

Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles 10.1038/s41598-017-05453-3

Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis 10.1038/s41598-017-11843-4 10.1038/s41598-017-11843-4.

Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays 10.1021/acschembio.7b00091

Host-pathogen systems for early drug discovery against tuberculosis 10.1016/j.mib.2017.11.017 10.1016/j.mib.2017.11.017.

Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages 10.1016/j.chom.2017.07.020 10.1016/j.chom.2017.07.020. Epub 2017 Aug 31.

Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling 10.1016/j.celrep.2017.08.101 10.1016/j.celrep.2017.08.101.

Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids 10.1073/pnas.1707840114 10.1073/pnas.1707840114.

Identification of Piperazinylbenzenesulfonamides as New Inhibitors of Claudin-1 Trafficking and Hepatitis C Virus Entry 10.1128/jvi.01982-17

Multiplexed Quantitation of Intraphagocyte Mycobacterium tuberculosis Secreted Protein Effectors 10.1016/j.celrep.2018.03.125

Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis 10.1016/j.bioorg.2018.08.025

Proteomics of Mycobacterium infection: Moving towards a Better Understanding of Pathogen-Driven immunomodulation 10.3389/fimmu.2018.00086

Synergy between circular bacteriocin AS-48 and ethambutol against Mycobacterium tuberculosis 10.1128/aac.00359-18

The EU approved antimalarial pyronaridine shows antitubercular activity and synergy with rifampicin, targeting RNA polymerase 10.1016/j.tube.2018.08.004

Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis 10.1038/s41598-017-11843-4

Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs 10.1016/j.ijpharm.2017.05.030

Host-pathogen systems for early drug discovery against tuberculosis 10.1016/j.mib.2017.11.017

Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages 10.1016/j.chom.2017.07.020

Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling 10.1016/j.celrep.2017.08.101

Phenotypic assays for Mycobacterium tuberculosis infection 10.1002/cyto.a.23129

A fast, fully automated cell segmentation algorithm for high-throughput and high-content screening 10.1002/cyto.a.20627

Compartmentalized Encapsulation of Two Antibiotics in Porous Nanoparticles: an Efficient Strategy to Treat Intracellular Infections 10.1002/ppsc.201800360

Spatiotemporal Changes of the Phagosomal Proteome in Dendritic Cells in Response to LPS Stimulation 10.1074/mcp.RA119.001316

Mycolactone as Analgesic: Subcutaneous Bioavailability Parameters 10.3389/fphar.2019.00378

Intrinsic Antibacterial Activity of Nanoparticles Made of β-Cyclodextrins Potentiates Their Effect as Drug Nanocarriers against Tuberculosis 10.1021/acsnano.8b07902

Mitochondrial Dynamics and Activity in Legionella-Infected Cells 10.1007/978-1-4939-9048-1_13

Heparin-Binding Hemagglutinin Adhesin (HBHA) Is Involved in Intracytosolic Lipid Inclusions Formation in Mycobacteria 10.3389/fmicb.2018.02258

Dehydrojuncusol, a Natural Phenanthrene Compound Extracted from Juncus maritimus, Is a New Inhibitor of Hepatitis C Virus RNA Replication 10.1128/jvi.02009-18

A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation 10.1039/C9OB00680J

Could Mycolactone Inspire New Potent Analgesics? Perspectives and Pitfalls 10.3390/toxins11090516

Paradoxical Roles of the MAL/Tirap Adaptor in Pathologies. 10.3389/fimmu.2020.569127

Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity. 10.1021/acsinfecdis.9b00277

Intracellular and in vivo evaluation of imidazo[2,1-b]thiazole-5-carboxamide anti-tuberculosis compounds. 10.1371/journal.pone.0227224

Preclinical assessment of a new live attenuated Mycobacterium tuberculosis Beijing-based vaccine for tuberculosis. 10.1016/j.vaccine.2019.11.085

IRG1 controls immunometabolic host response and restricts intracellular Mycobacterium tuberculosis infection 10.1101/761551

Worms' Antimicrobial Peptides. 10.3390/md17090512

T(oo)bAd. 10.1038/s41589-019-0347-x

Theaflavins, polyphenols of black tea, inhibit entry of hepatitis C virus in cell culture. 10.1371/journal.pone.0198226

Plant extracts from Cameroonian medicinal plants strongly inhibit hepatitis C virus infection in vitro. 10.3389/fmicb.2015.00488

Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis. 10.1038/nm.3262

Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis. 10.1021/jm300377g

Shortening the drug discovery pipeline: small molecule high content screening for lead discovery in neglected disease. 10.1186/1753-6561-5-s1-p38

Automated HTS/HCS for antivirals using visual HIV full replication assays. 10.1186/1742-4690-6-s2-p82

Influence of ESAT-6 secretion system 1 (RD1) of Mycobacterium tuberculosis on the interaction between mycobacteria and the host immune system. 10.4049/jimmunol.174.6.3570

Cell microbiology interview 10.1111/cmi.13288

Pathogenomic analyses of Mycobacterium microti, an ESX-1-deleted member of the Mycobacterium tuberculosis complex causing disease in various hosts 10.1099/mgen.0.000505

Maria Paola Costi

Costi Maria Paola

ORCID: 0000-0002-0443-5402

2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1 10.1021/cb5007163

Alanine Mutants of the Interface Residues of Human Thymidylate Synthase Decode Key Features of the Binding Mode of Allosteric Anticancer Peptides 10.1021/jm5011176

Hotspots in an Obligate Homodimeric Anticancer Target. Structural and Functional Effects of Interfacial Mutations in Human Thymidylate Synthase 10.1021/acs.jmedchem.5b00137

Theoretical analysis of the addition of hydroxylamine to uracil and 5-fluorouracil as a model for the thymidylate synthase reaction (vol 343, pg 1, 1995) 10.1016/j.comptc.2014.03.012

2- N-Alkyl(R-phenyl)-aminomethyl -3-phenyl-7-trifluoromethylquinoxalines as anticancer agents inhibitors of folate enzymes 10.1016/j.ejmech.2014.01.048

Internalization and Stability of a Thymidylate Synthase Peptide Inhibitor in Ovarian Cancer Cells 10.1021/jm501397h

Mass Spectrometric/Bioinformatic Identification of a Protein Subset That Characterizes the Cellular Activity of Anticancer Peptides 10.1021/pr500510v

Optimization of Peptides That Target Human Thymidylate Synthase to Inhibit Ovarian Cancer Cell Growth 10.1021/jm401574p

Targeting class A and C serine β-lactamases with a broad-spectrum boronic acid derivative 10.1021/jm5006572

2 '-Deoxyuridine 5 '-Monophosphate Substrate Displacement in Thymidylate Synthase through 6-Hydroxy-2H-naphtho 1,8-bc furan-2-one Derivatives 10.1021/jm4014086

Biochemical effects of riluzole on Leishmania parasites 10.1016/j.exppara.2012.11.013

Discovery of highly potent acid ceramidase inhibitors with in vitro tumor chemosensitizing activity 10.1038/srep01035

Ligand-based discovery of N-(1,3-dioxo-1H,3H-benzo de isochromen-5-yl)-carboxamide and sulfonamide derivatives as thymidylate synthase A inhibitors 10.1016/j.bmcl.2012.11.117

Modulation of the expression of folate cycle enzymes and polyamine metabolism by berberine in cisplatin-sensitive and-resistant human ovarian cancer cells 10.3892/ijo.2013.2045

Translational repression of thymidylate synthase by targeting its mRNA 10.1093/nar/gkt098

Biological evaluation of MR36, a novel non-polyglutamatable thymidylate synthase inhibitor that blocks cell cycle progression in melanoma cell lines 10.1007/s10637-011-9733-2

Distamycin A and derivatives as synergic drugs in cisplatin-sensitive and -resistant ovarian cancer cells 10.1007/s00726-011-1039-3

Inhibitor of Ovarian Cancer Cells Growth by Virtual Screening: A New Thiazole Derivative Targeting Human Thymidylate Synthase 10.1021/jm300850v

Structure-Based Selectivity Optimization of Piperidine-Pteridine Derivatives as Potent Leishmania Pteridine Reductase Inhibitors 10.1021/jm300563f

The structure of Enterococcus faecalis thymidylate synthase provides clues about folate bacterial metabolism 10.1107/s0907444912026236

Identification of the Binding Modes of N-Phenylphthalimides Inhibiting Bacterial Thymidylate Synthase through X-Ray Crystallography Screening 10.1021/jm2005018

Permeation through the cell membrane of a boron-based β-lactamase inhibitor 10.1371/journal.pone.0023187

Protein-protein interface-binding peptides inhibit the cancer therapy target human thymidylate synthase 10.1073/pnas.1104829108

Virtual Screening Identification of Nonfolate Compounds, Including a CNS Drug, as Antiparasitic Agents Inhibiting Pteridine Reductase 10.1021/jm1010572

Design and characterization of a mutation outside the active site of human thymidylate synthase that affects ligand binding 10.1093/protein/gzp075

Dimer-monomer equilibrium of human thymidylate synthase monitored by fluorescence resonance energy transfer 10.1002/pro.379

Drug resistance in ovarian cancer: Biomarkers and treatments Highlights from the DROC meeting held in Modena (Italy) on the 19th and 20th of February 2009. Scientific topics discussed at the meeting are reported in the present issue 10.1016/j.ygyno.2010.03.006

Ligand-based virtual screening and ADME-tox guided approach to identify triazolo-quinoxalines as folate cycle inhibitors 10.1016/j.bmc.2010.09.065

Novel Approaches for Targeting Thymidylate Synthase To Overcome the Resistance and Toxicity of Anticancer Drugs 10.1021/jm901869w

Spermidine/spermine N1-acetyltranferase modulation by novel folate cycle inhibitors in cisplatin-sensitive and -resistant human ovarian cancer cell lines 10.1016/j.ygyno.2009.11.030

Structural study of phenyl boronic acid derivatives as AmpC β-lactamase inhibitors 10.1016/j.bmcl.2010.04.007

Anchors away 10.1038/458840a

Collateral sensitivity to novel thymidylate synthase inhibitors correlates with folate cycle enzymes impairment in cisplatin-resistant human ovarian cancer cells 10.1016/j.ejphar.2009.04.062

Comprehensive mechanistic analysis of hits from high-throughput and docking screens against β-lactamase 10.1021/jm701500e

Constrained dansyl derivatives reveal bacterial specificity of high conserved thymidylate synthases 10.1002/cbic.200700524

Discovery of potent pteridine reductase inhibitors to guide antiparasite drug development 10.1073/pnas.0704384105

Opening opportunities for new drugs against neglected diseases 10.1002/cmdc.200800036

Sequence-based identification of specific drug target regions in the thymidylate synthase enzyme family 10.1002/cmdc.200700215

Synthesis of N-(5,7-diamino-3-phenyl-quinoxalin-2-yl)-3,4,5-substituted anilines and N- 4 (5,7-diamino-3-phenylquinoxalin-2-yl)amino benzoyl -L-glutamic acid diethyl ester: Evaluation of in vitro anti-cancer and anti-folate activities 10.1016/j.ejmech.2007.03.035

New thymidylate synthase inhibitors induce apoptosis in melanoma cell lines 10.1016/j.tiv.2006.09.023

Optimizing cell permeation of an antibiotic resistance inhibitor for improved efficacy 10.1021/jm070643q

Antibacterial agent discovery using thymidylate synthase biolibrary screening 10.1021/jm051187d

Combination of suboptimal doses of inhibitors targeting different domains of LtrMDR1 efficiently overcomes resistance of Leishmania spp. to miltefosine by inhibiting drug efflux 10.1128/aac.00423-06

Improving specificity vs bacterial thymidylate synthases through N-dansyl modulation of didansyltyrosine 10.1021/jm0491445

The structure of Cryptococcus neoformans thymidylate synthase suggests strategies for using target dynamics for species-specific inhibition 10.1107/s0907444905022638

Thymidylate synthase structure, function and implication in drug discovery 10.2174/0929867054864868

Aza-boronic acids as non-β-lactam inhibitors of AmpC-β-lactamase 10.1016/j.bmcl.2004.05.054

Inhibitor specificity via protein dynamics: Insights from the design of antibacterial agents targeted against thymidylate synthase 10.1016/j.chembiol.2003.11.012

ortho-halogen naphthaleins as specific inhibitors of Lactobacillus casei thymidylate synthase. Conformational properties and biological activity 10.1016/s0968-0896(02)00541-2

The structural roles of conserved Pro196, Pro197 and His199 in the mechanism of thymidylate synthase 10.1093/protein/gzg076

Structure-based studies on species-specific inhibition of thymidylate synthase 10.1016/s0925-4439(02)00083-2

Predicting and harnessing protein flexibility in the design of species-specific inhibitors of thymidylate synthase 10.1016/s1074-5521(01)00067-9

Structure-based design and in-parallel synthesis of inhibitors of AmpC beta-lactamase 10.1016/s1074-5521(01)00034-5

Update on antifolate drugs targets 10.2174/1389450013348669

Structures and reactivities of 1-oxo-cycloalkan-2-ylideneacetic acids. A H-1 NMR, modelling and photochemical study 10.1016/s0040-4020(00)00662-1

Phthalein derivatives as a new tool for selectivity in thymidylate synthase inhibition 10.1021/jm9900016

Structure-based design of inhibitors specific for bacterial thymidylate synthase 10.1021/bi9815896

Structure-based discovery and in-parallel optimization of novel competitive inhibitors of thymidylate synthase 10.1016/s1074-5521(99)80077-5

Quinoxaline chemistry. Part 11. 3-phenyl-2 phenoxy- and phenoxymethyl -6(7) or 6,8-substituted quinoxalines and N- 4-(6(7)-substituted or 6,8-disubstituted-3-phenylquinoxalin-2-yl)hydroxy or hydroxymethyl benzoylglutamates. Synthesis and evaluation of in vitro anticancer activity and enzymatic inhibitory activity against dihydrofolate reductase and thymidylate synthase 10.1016/s0014-827x(98)00054-8

Thymidylate synthase inhibition: A structure-based rationale for drug design (vol 18, pg 21, 1998) 10.1002/(sici)1098-1128(199805)18:3<187::aid-med3>3.0.co;2-t

Asparagine 229 mutants of thymidylate synthase catalyze the methylation of 3-methyl-2'-deoxyuridine 5'-monophosphate 10.1021/bi952642i

Conformational analysis of phthalein derivatives acting as thymidylate synthase inhibitors by means of 1H NMR and quantum chemical calculations 10.1016/0968-0896(96)00193-9

Naphthalimido derivatives as antifolate thymidylate synthase inhibitors 10.1016/s0223-5234(97)86180-6

A condensed thiadiazolo-pyrimidine as a new efficient fluorophore. Theoretical and experimental investigation of the electronic spectra and photophysics 10.1016/1010-6030(94)80047-2

THEORETICAL-STUDY OF ELECTRONIC-SPECTRA AND PHOTOPHYSICS OF URACIL DERIVATIVES 10.1111/j.1751-1097.1990.tb04192.x

Long period fiber grating biosensor for the detection of drug resistant bacteria: The 'OPTObacteria' project 10.1109/MePhoCo.2014.6866453

The inhibition of extended spectrum β-lactamases: Hits and leads 10.2174/09298673113206660323

Targeting the Trypanosomatidic Enzymes Pteridine Reductase and Dihydrofolate Reductase 10.1002/9783527670383.ch24

A primary pulmonary artery chondrosarcoma manifesting as acute pulmonary embolism 10.1016/j.athoracsur.2012.03.108

Homodimeric enzymes as drug targets 10.2174/092986710790712156

Novel 3-benzoyl-2-piperazinylquinoxaline derivatives as potential antitumor agents 10.1002/jhet.5570430304

Structure-based optimization of a non-β-lactam lead results in inhibitors that do not up-regulate β-lactamase expression in cell culture 10.1021/ja042984o

Quinoxaline chemistry. Part 15. 4-[2-Quinoxalylmethylenimino]- benzoylglutamates and -benzoates, 4-[2-quinoxalylmethyl-N-methylamino]- benzoylglutamates as analogues of classical antifolate agents. Synthesis, elucidation of structures and in vitro evaluation of antifolate and anticancer activities 10.1016/S0014-827X(02)00005-8

Theoretical analysis of the addition of hydroxylamine to uracil and 5-fluorouracil as a model for the thymidylate synthase reaction 10.1016/0166-1280(95)90513-8

Comparing Drug Images and Repurposing Drugs with BioGPS and FLAPdock: The Thymidylate Synthase Case 10.1002/cmdc.201600121

Chroman-4-One Derivatives Targeting Pteridine Reductase 1 and Showing Anti-Parasitic Activity 10.3390/molecules22030426

Repurposing of Drugs Targeting YAP-TEAD Functions 10.3390/cancers10090329

Structural Comparison of Enterococcus faecalis and Human Thymidylate Synthase Complexes with the Substrate dUMP and Its Analogue FdUMP Provides Hints about Enzyme Conformational Variabilities 10.3390/molecules24071257

Structural and Functional Characterization of the Human Thymidylate Synthase (hTS) Interface Variant R175C, New Perspectives for the Development of hTS Inhibitors 10.3390/molecules24071362

Structural Insights into the Development of Cycloguanil Derivatives as Trypanosoma brucei Pteridine-Reductase-1 Inhibitors 10.1021/acsinfecdis.8b00358

Cyclic Peptides Acting as Allosteric Inhibitors of Human Thymidylate Synthase and Cancer Cell Growth 10.3390/molecules24193493

The 1,10-Phenanthroline Ligand Enhances the Antiproliferative Activity of DNA-Intercalating Thiourea-Pd(II) and -Pt(II) Complexes Against Cisplatin-Sensitive and -Resistant Human Ovarian Cancer Cell Lines 10.3390/ijms20246122

Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology 10.1021/acs.jmedchem.9b01456

New Insights into Bioactive Compounds from the Medicinal Plant Spathodea campanulata P. Beauv. and Their Activity against Helicobacter pylori 10.3390/antibiotics9050258

High-resolution crystal structure of Trypanosoma brucei pteridine reductase 1 in complex with an innovative tricyclic-based inhibitor 10.1107/S2059798320004891

A Peptidic Thymidylate-Synthase Inhibitor Loaded on Pegylated Liposomes Enhances the Antitumour Effect of Chemotherapy Drugs in Human Ovarian Cancer Cells 10.3390/ijms21124452

Structural Bases for the Synergistic Inhibition of Human Thymidylate Synthase and Ovarian Cancer Cell Growth by Drug Combinations 10.3390/cancers13092061

Evidence of Pyrimethamine and Cycloguanil Analogues as Dual Inhibitors of Trypanosoma brucei Pteridine Reductase and Dihydrofolate Reductase 10.3390/ph14070636

Design, Synthesis and Antiparasitic Evaluation of Click Phospholipids 10.3390/molecules26144204

João Neres

Neres João

ORCID: 0000-0003-4488-2423

http://www.linkedin.com/in/joaoneres

Insights into the Activity and Specificity of Trypanosoma cruzi trans-Sialidase from Molecular Dynamics Simulations 10.1021/bi301112p

Non-Nucleoside Inhibitors of BasE, an Adenylating Enzyme in the Siderophore Biosynthetic Pathway of the Opportunistic Pathogen Acinetobacter baumannii 10.1021/jm301709s

Structural Basis for Benzothiazinone-Mediated Killing of Mycobacterium tuberculosis 10.1126/scitranslmed.3004395

Towards a new tuberculosis drug: pyridomycin - nature's isoniazid 10.1002/emmm.201201689

Biochemical and Structural Characterization of Bisubstrate Inhibitors of BasE, the Self-Standing Nonribosomal Peptide Synthetase Adenylate-Forming Enzyme of Acinetobactin Synthesis 10.1021/bi101226n

Biological and structural characterization of the Mycobacterium smegmatis nitroreductase NfnB, and its role in benzothiazinone resistance 10.1111/j.1365-2958.2010.07277.x

Biophysical and X-ray Crystallographic Analysis of Mps1 Kinase Inhibitor Complexes 10.1021/bi901970c

Inhibitors of the Salicylate Synthase (MbtI) from Mycobacterium tuberculosis Discovered by High-Throughput Screening 10.1002/cmdc.201000275

Tryptophan as a Molecular Shovel in the Glycosyl Transfer Activity of Trypanosoma cruzi Trans-sialidase 10.1016/j.bpj.2010.01.006

Discovery of novel inhibitors of Trypanosoma cruzi trans-sialidase from in silico screening 10.1016/j.bmcl.2008.12.065

The Global Virulence Regulators VsrAD and PhcA Control Secondary Metabolism in the Plant Pathogen Ralstonia solanacearum 10.1002/cbic.200900510

Aryl Acid Adenylating Enzymes Involved in Siderophore Biosynthesis: Fluorescence Polarization Assay, Ligand Specificity, and Discovery of Non-nucleoside Inhibitors via High-Throughput Screening 10.1021/bi801625b

Inhibition of Siderophore Biosynthesis by 2-Triazole Substituted Analogues of 5'-O-[N-(Salicyl)sulfamoyl]adenosine: Antibacterial Nucleosides Effective against Mycobacterium tuberculosis 10.1021/jm8008037

Inhibition of siderophore biosynthesis in Mycobacterium tuberculosis with nucleoside bisubstrate analogues: Structure-activity relationships of the nucleobase domain of 5 '-O-[N-(salicyl)sulfamoyl]adenosine 10.1021/jm800567v

Rational drug design in parasitology: trans-sialidase as a case study for Chagas disease 10.1016/j.drudis.2007.12.004

Benzoic acid and pyridine derivatives as inhibitors of Trypanosoma cruzi trans-sialidase 10.1016/j.bmc.2006.12.024

Continuous fluorimetric assay for high-throughput screening of inhibitors of trans-sialidase from Trypanosoma cruzi 10.1016/j.ab.2006.07.018

Towards a new combination therapy for tuberculosis with next generation benzothiazinones 10.1002/emmm.201303575

Selective detection of epimeric pentose saccharides at physiological pH using a fluorescent receptor 10.1016/j.carres.2014.02.007

Pyridomycin bridges the NADH- and substrate-binding pockets of the enoyl reductase InhA 10.1038/nchembio.1405

2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1 10.1021/cb5007163

Discovery of benzothiazoles as antimycobacterial agents: Synthesis, structure–activity relationships and binding studies with Mycobacterium tuberculosis decaprenylphosphoryl-β-d-ribose 2′-oxidase 10.1016/j.bmc.2015.11.017

Mechanism of a Standalone β‐Lactone Synthetase: New Continuous Assay for a Widespread ANL Superfamily Enzyme 10.1002/cbic.201800821

Nathalie deboosere

deboosere Nathalie

ORCID: 0000-0002-2873-5485

ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton. 10.15252/embr.201744371

Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling. 10.1016/j.celrep.2017.08.101

A Bacterial Toxin with Analgesic Properties: Hyperpolarization of DRG Neurons by Mycolactone. 10.3390/toxins9070227

Phenotypic assays for Mycobacterium tuberculosis infection. 10.1002/cyto.a.23129

Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays. 10.1021/acschembio.7b00091

STAT3 Represses Nitric Oxide Synthesis in Human Macrophages upon Mycobacterium tuberculosis Infection. 10.1038/srep29297

LppM impact on the colonization of macrophages by Mycobacterium tuberculosis. 10.1111/cmi.12619

A microscopic phenotypic assay for the quantification of intracellular mycobacteria adapted for high-throughput/high-content screening. 10.3791/51114

Adhesion of human pathogenic enteric viruses and surrogate viruses to inert and vegetal food surfaces. 10.1016/j.fm.2012.04.007

Viral elution and concentration method for detection of influenza A viruses in mud by real-time RT-PCR. 10.1016/j.jviromet.2011.10.013

Comparison of chlorine and peroxyacetic-based disinfectant to inactivate Feline calicivirus, Murine norovirus and Hepatitis A virus on lettuce. 10.1016/j.ijfoodmicro.2011.08.011

Direct detection of highly pathogenic avian influenza A/H5N1 virus from mud specimens. 10.1016/j.jviromet.2011.06.002

Development and validation of a concentration method for the detection of influenza a viruses from large volumes of surface water. 10.1128/aem.02484-10

A predictive microbiology approach for thermal inactivation of Hepatitis A virus in acidified berries. 10.1016/j.fm.2010.05.018

Assessment of the removal and inactivation of influenza viruses H5N1 and H1N1 by drinking water treatment. 10.1016/j.watres.2010.01.013

Intra-laboratory validation of a concentration method adapted for the enumeration of infectious F-specific RNA coliphage, enterovirus, and hepatitis A virus from inoculated leaves of salad vegetables. 10.1016/j.ijfoodmicro.2005.11.007

Modelling effect of physical and chemical parameters on heat inactivation kinetics of hepatitis A virus in a fruit model system. 10.1016/j.ijfoodmicro.2003.10.015

Host-pathogen systems for early drug discovery against tuberculosis. 10.1016/j.mib.2017.11.017

Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids. 10.1073/pnas.1707840114

Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis. 10.1038/s41598-017-11843-4

Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages. 10.1016/j.chom.2017.07.020

Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles. 10.1038/s41598-017-05453-3

Host-directed therapies offer novel opportunities for the fight against tuberculosis. 10.1016/j.drudis.2017.05.005

Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs. 10.1016/j.ijpharm.2017.05.030

Impact of pe_pgrs33 Gene Polymorphisms on Mycobacterium tuberculosis Infection and Pathogenesis. 10.3389/fcimb.2017.00137

Clofazimine encapsulation in nanoporous silica particles for the oral treatment of antibiotic-resistant Mycobacterium tuberculosis infections. 10.2217/nnm-2016-0364

Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420. 10.1126/science.aag1006

How can nanoparticles contribute to antituberculosis therapy? 10.1016/j.drudis.2017.01.011

Genome-wide, high-content siRNA screening identifies the Alzheimer's genetic risk factor FERMT2 as a major modulator of APP metabolism. 10.1007/s00401-016-1652-z

Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria. 10.1111/mmi.13535

Mycobacterium tuberculosis LppM Displays an Original Structure and Domain Composition Linked to a Dual Localization. 10.1016/j.str.2016.07.009

Khaya grandifoliola C.DC: a potential source of active ingredients against hepatitis C virus in vitro. 10.1007/s00705-016-2771-5

[Mycolactone: the amazing analgesic mycobacterial toxin]. 10.1051/medsci/20163202007

A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters. 10.1039/c5ob02630j

Polyphenols Inhibit Hepatitis C Virus Entry by a New Mechanism of Action. 10.1128/jvi.01473-15

Plant extracts from Cameroonian medicinal plants strongly inhibit hepatitis C virus infection in vitro. 10.3389/fmicb.2015.00488

Increased protective efficacy of recombinant BCG strains expressing virulence-neutral proteins of the ESX-1 secretion system. 10.1016/j.vaccine.2015.03.083

Cytosolic access of Mycobacterium tuberculosis: critical impact of phagosomal acidification control and demonstration of occurrence in vivo. 10.1371/journal.ppat.1004650

[High content screening in chemical biology: overview and main challenges]. 10.1051/medsci/20153102016

Testing chemical and genetic Modulators in Mycobacterium tuberculosis infected cells using phenotypic assays. 10.1007/978-1-4939-2450-9_24

2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1. 10.1021/cb5007163

High-content screening technology combined with a human granuloma model as a new approach to evaluate the activities of drugs against Mycobacterium tuberculosis. 10.1128/aac.03705-14

Mycobacterial toxin induces analgesia in buruli ulcer by targeting the angiotensin pathways. 10.1016/j.cell.2014.04.040

Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches. 10.1021/jm500422b

Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis. 10.1038/nm.3262

The balance of apoptotic and necrotic cell death in Mycobacterium tuberculosis infected macrophages is not dependent on bacterial virulence. 10.1371/journal.pone.0047573

Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis. 10.1021/jm300377g

Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors. 10.1021/jm200825u

A novel specific edge effect correction method for RNA interference screenings. 10.1093/bioinformatics/btr648

Analogous mechanisms of resistance to benzothiazinones and dinitrobenzamides in Mycobacterium smegmatis. 10.1371/journal.pone.0026675

High-content screening in infectious diseases. 10.1016/j.cbpa.2011.05.023

Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors. 10.1021/jm200076a

Shortening the drug discovery pipeline: small molecule high content screening for lead discovery in neglected disease. 10.1186/1753-6561-5-s1-p38

High content phenotypic cell-based visual screen identifies Mycobacterium tuberculosis acyltrehalose-containing glycolipids involved in phagosome remodeling. 10.1371/journal.ppat.1001100

High-content imaging of Mycobacterium tuberculosis-infected macrophages: an in vitro model for tuberculosis drug discovery. 10.4155/fmc.10.223

Functional characterization of the Mycobacterium tuberculosis serine/threonine kinase PknJ. 10.1099/mic.0.038133-0

High content screening identifies decaprenyl-phosphoribose 2' epimerase as a target for intracellular antimycobacterial inhibitors. 10.1371/journal.ppat.1000645

Systematic genetic nomenclature for type VII secretion systems. 10.1371/journal.ppat.1000507

Long-circulating DNA lipid nanocapsules as new vector for passive tumor targeting. 10.1016/j.biomaterials.2009.09.044

Automated HTS/HCS for antivirals using visual HIV full replication assays. 10.1186/1742-4690-6-s2-p82

Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis. 10.1126/science.1171583

Automated high-throughput siRNA transfection in raw 264.7 macrophages: a case study for optimization procedure. 10.1177/1087057108328762

Control of M. tuberculosis ESAT-6 secretion and specific T cell recognition by PhoP. 10.1371/journal.ppat.0040033

ESAT-6 from Mycobacterium tuberculosis dissociates from its putative chaperone CFP-10 under acidic conditions and exhibits membrane-lysing activity. 10.1128/jb.00469-07

[Aquatic insects and transmission of Mycobacterium ulcerans]. 10.1051/medsci/20072367572

Impact of Mycobacterium ulcerans biofilm on transmissibility to ecological niches and Buruli ulcer pathogenesis. 10.1371/journal.ppat.0030062

Protection against Mycobacterium ulcerans lesion development by exposure to aquatic insect saliva. 10.1371/journal.pmed.0040064

Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues. 10.1016/j.bmc.2006.12.009

Inactivation of Rv2525c, a substrate of the twin arginine translocation (Tat) system of Mycobacterium tuberculosis, increases beta-lactam susceptibility and virulence. 10.1128/jb.00631-06

High frequency of CD4+ T cells specific for the TB10.4 protein correlates with protection against Mycobacterium tuberculosis infection. 10.1128/iai.02086-05

Benzofuro[3,2-f][1]benzopyrans: a new class of antitubercular agents. 10.1016/j.bmc.2006.03.033

An increase in antimycobacterial Th1-cell responses by prime-boost protocols of immunization does not enhance protection against tuberculosis. 10.1128/iai.74.4.2128-2137.2006

Dissection of ESAT-6 system 1 of Mycobacterium tuberculosis and impact on immunogenicity and virulence. 10.1128/iai.74.1.88-98.2006

Tuberculosis: from genome to vaccine. 10.1586/14760584.4.4.541

Functional analysis of early secreted antigenic target-6, the dominant T-cell antigen of Mycobacterium tuberculosis, reveals key residues involved in secretion, complex formation, virulence, and immunogenicity. 10.1074/jbc.m503515200

Immunogenic membrane-associated proteins of Mycobacterium tuberculosis revealed by proteomics. 10.1099/mic.0.27799-0

Influence of ESAT-6 secretion system 1 (RD1) of Mycobacterium tuberculosis on the interaction between mycobacteria and the host immune system. 10.4049/jimmunol.174.6.3570

Evaluation of vaccines in the EU TB Vaccine Cluster using a guinea pig aerosol infection model of tuberculosis. 10.1016/j.tube.2004.09.009

ESAT-6 proteins: protective antigens and virulence factors? 10.1016/j.tim.2004.09.007

Enhanced protection against tuberculosis by vaccination with recombinant Mycobacterium microti vaccine that induces T cell immunity against region of difference 1 antigens. 10.1086/421468

Cell envelope protein PPE68 contributes to Mycobacterium tuberculosis RD1 immunogenicity independently of a 10-kilodalton culture filtrate protein and ESAT-6. 10.1128/iai.72.4.2170-2176.2004

Macro-array and bioinformatic analyses reveal mycobacterial 'core' genes, variation in the ESAT-6 gene family and new phylogenetic markers for the Mycobacterium tuberculosis complex. 10.1099/mic.0.26662-0

CD8+-T-cell responses of Mycobacterium-infected mice to a newly identified major histocompatibility complex class I-restricted epitope shared by proteins of the ESAT-6 family. 10.1128/iai.71.12.7173-7177.2003

Recombinant BCG exporting ESAT-6 confers enhanced protection against tuberculosis. 10.1038/nm859

Loss of RD1 contributed to the attenuation of the live tuberculosis vaccines Mycobacterium bovis BCG and Mycobacterium microti. 10.1046/j.1365-2958.2002.03237.x

Bacterial artificial chromosome-based comparative genomic analysis identifies Mycobacterium microti as a natural ESAT-6 deletion mutant. 10.1128/iai.70.10.5568-5578.2002

Disruption of HIV-1 integrase-DNA complexes by short 6-oxocytosine-containing oligonucleotides. 10.1021/bi015732y

IRG1 controls immunometabolic host response and restricts intracellular Mycobacterium tuberculosis infection 10.1101/761551

Large scale screening discovers clofoctol as an inhibitor of SARS-CoV-2 replication that reduces COVID-19-like pathology 10.1101/2021.06.30.450483

Ruben Hartkoorn

Hartkoorn Ruben / Ruben C. Hartkoorn

ORCID: 0000-0001-7315-1553

A druggable secretory protein maturase of Toxoplasma essential for invasion and egress 10.7554/eLife.27480

Discovery and Biosynthesis of Gladiolin: A Burkholderia gladioli Antibiotic with Promising Activity against Mycobacterium tuberculosis 10.1021/jacs.7b03382

Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria 10.1111/mmi.13535

MoS2/TiO2/SiNW surface as an effective substrate for LDI-MS detection of glucose and glutathione in real samples 10.1016/j.talanta.2017.04.061

The Inosine Monophosphate Dehydrogenase, GuaB2, Is a Vulnerable New Bactericidal Drug Target for Tuberculosis 10.1021/acsinfecdis.6b00102

Micrococcin P1-A bactericidal thiopeptide active against Mycobacterium tuberculosis 10.1016/j.tube.2016.07.011

2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1 10.1021/cb5007163

Bioluminescence for Assessing Drug Potency against Nonreplicating Mycobacterium tuberculosis 10.1128/aac.00528-15

Lead selection and characterization of antitubercular compounds using the Nested Chemical Library 10.1016/j.tube.2015.02.028

The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis 10.1128/aac.00778-15

Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG 10.1016/j.chembiol.2015.05.016

Whole cell screen based identification of spiropiperidines with potent antitubercular properties 10.1016/j.bmcl.2015.05.087

Anticytolytic Screen Identifies Inhibitors of Mycobacterial Virulence Protein Secretion 10.1016/j.chom.2014.09.008

Assessing the essentiality of the decaprenyl-phospho-D-arabinofuranose pathway in Mycobacterium tuberculosis using conditional mutants 10.1111/mmi.12546

Cross-Resistance between Clofazimine and Bedaquiline through Upregulation of MmpL5 in Mycobacterium tuberculosis 10.1128/aac.00037-14

Mechanism of Action of 5-Nitrothiophenes against Mycobacterium tuberculosis 10.1128/aac.02693-13

Rv2466c Mediates the Activation of TP053 To Kill Replicating and Non-replicating Mycobacterium tuberculosis 10.1021/cb500149m

Towards a new combination therapy for tuberculosis with next generation benzothiazinones 10.1002/emmm.201303575

Synthesis and Antimycobacterial Activity of 2,1 '-Dihydropyridomycins 10.1021/ml300385q

Genome-Wide Definition of the SigF Regulon in Mycobacterium tuberculosis 10.1128/jb.06692-11

In Vitro Combination Studies of Benzothiazinone Lead Compound BTZ043 against Mycobacterium tuberculosis 10.1128/aac.01476-12

Streptomycin-Starved Mycobacterium tuberculosis 18b, a Drug Discovery Tool for Latent Tuberculosis 10.1128/aac.01125-12

Towards a new tuberculosis drug: pyridomycin - nature's isoniazid 10.1002/emmm.201201689

Virulence Regulator EspR of Mycobacterium tuberculosis Is a Nucleoid-Associated Protein 10.1371/journal.ppat.1002621

Tuberculosis drugs: new candidates and how to find more 10.2217/fmb.11.46

HIV protease inhibitors are substrates for OATP1A2, OATP1B1 and OATP1B3 and lopinavir plasma concentrations are influenced by SLCO1B1 polymorphisms 10.1097/FPC.0b013e328335b02d

Leads for antitubercular compounds from kinase inhibitor library screens 10.1016/j.tube.2010.09.001

Sigma Factor F Does Not Prevent Rifampin Inhibition of RNA Polymerase or Cause Rifampin Tolerance in Mycobacterium tuberculosis 10.1128/jb.00687-10

Simple Model for Testing Drugs against Nonreplicating Mycobacterium tuberculosis 10.1128/aac.00821-10

Intracellular 'boosting' of darunavir using known transport inhibitors in primary PBMC 10.1111/j.1365-2125.2009.03462.x

Intracellular accumulation of efavirenz and nevirapine is independent of P-glycoprotein activity in cultured CD4 T cells and primary human lymphocytes 10.1093/jac/dkp335

Cultured CD4T cells and primary human lymphocytes express hOATPs: intracellular accumulation of saquinavir and lopinavir 10.1038/bjp.2008.320

A rapid and sensitive HPLC-MS method for the detection of plasma and cellular rifampicin 10.1016/j.jchromb.2007.07.005

Differential drug susceptibility of intracellular and extracellular tuberculosis, and the impact of P-glycoprotein 10.1016/j.tube.2006.12.001

Tacrine-induced liver damage: an analysis of 19 candidate genes 10.1097/FPC.0b013e3282f1f12b

Down regulation of multidrug resistance protein-1 expression in patients with early rheumatoid arthritis exposed to methotrexate as a first disease-modifying antirheumatic drug 10.1136/ard.2005.049189

Low levels of pyrazinamide and ethambutol in children with tuberculosis and impact of age, nutritional status, and human immunodeficiency virus infection 10.1128/aac.50.2.407-413.2006

In vitro synergy and enhanced murine brain penetration of saquinavir coadministered with mefloquine 10.1124/jpet..105.086272

Modulation of the intracellular accumulation of saquinavir in peripheral blood mononuclear cells by inhibitors of MRP1, MRP2, P-gp and BCRP 10.1097/01.aids.0000194793.36175.40

Expression of P-glycoprotein, multidrug-resistance proteins 1 and 2 in CEM, CEMVBL, CEME1000, MDCKIIMRP1 and MDCKIIMRP2 cell lines 10.1097/01.aids.0000088212.77946.65

Pyrrolomycins Are Potent Natural Protonophores 10.1128/AAC.01450-19

Intragenic Distribution of IS 6110 in Clinical Mycobacterium tuberculosis Strains: Bioinformatic Evidence for Gene Disruption Leading to Underdiagnosed Antibiotic Resistance 10.1128/Spectrum.00019-21

Giorgia Mori

Mori Giorgia

ORCID: 0000-0003-3469-5632

Pyridine-3,4-dicarboximide as starting material for the total synthesis of the natural product eupolauramine and its isomer iso-eupolauramine endowed with anti-tubercular activities 10.1016/j.tet.2015.01.034

DprE1, a new taxonomic marker in mycobacteria 10.1111/1574-6968.12246

Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth 10.1016/j.ejmech.2015.06.035

Analogous mechanisms of resistance to benzothiazinones and dinitrobenzamides in Mycobacterium smegmatis 10.1371/journal.pone.0026675

Synthesis of 3-heteryl substituted pyrrolidine-2,5-diones via catalytic Michael reaction and evaluation of their inhibitory activity against InhA and Mycobacterium tuberculosis 10.1016/j.ejmech.2013.10.069

New prodrugs against tuberculosis 10.1016/j.drudis.2016.09.006

Evaluation of the inhibitory activity of (aza)isoindolinone-type compounds: toward in vitro InhA action, Mycobacterium tuberculosis growth and mycolic acid biosynthesis 10.1111/cbdd.12804

Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG 10.1016/j.chembiol.2015.05.016

Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043 10.1021/acsmedchemlett.5b00424

Rv2466c mediates the activation of TP053 to kill replicating and non-replicating Mycobacterium tuberculosis 10.1021/cb500149m

Pyrrolidinone and pyrrolidine derivatives: Evaluation as inhibitors of InhA and Mycobacterium tuberculosis 10.1016/j.ejmech.2016.07.028

Triazolophthalazines: Easily Accessible Compounds with Potent Antitubercular Activity 10.1002/cmdc.201600085

2-carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1 10.1021/cb5007163

New and old hot drug targets in tuberculosis 10.2174/1389557516666160831164925

A Phenotypic Based Target Screening Approach Delivers New Antitubercular CTP Synthetase Inhibitors 10.1021/acsinfecdis.7b00006

Mechanochemical synthesis and biological evaluation of novel isoniazid derivatives with potent antitubercular activity 10.3390/molecules22091457

Evaluation of heteroatom-rich derivatives as antitubercular agents with InhA inhibition properties 10.1007/s00044-017-2064-x

Shifts of Faecal Microbiota during Sporadic Colorectal Carcinogenesis 10.1038/s41598-018-28671-9

Discovery and development of novel salicylate synthase (MbtI) furanic inhibitors as antitubercular agents 10.1016/j.ejmech.2018.06.033

The EU approved antimalarial pyronaridine shows antitubercular activity and synergy with rifampicin, targeting RNA polymerase 10.1016/j.tube.2018.08.004

A multitarget approach to drug discovery inhibiting Mycobacterium tuberculosis PyrG and PanK 10.1038/s41598-018-21614-4

Synthesis, oxidation potential and anti–mycobacterial activity of isoniazid and analogues: insights into the molecular isoniazid activation mechanism 10.1002/slct.201600040

Gut microbiota analysis in postoperative lynch syndrome patients 10.3389/fmicb.2019.01746

Gut Microbial Signatures in Sporadic and Hereditary Colorectal Cancer 10.3390/ijms22031312

2-Aminooxazole as a Novel Privileged Scaffold in Antitubercular Medicinal Chemistry. 10.1021/acsmedchemlett.0c00173

Rv0579 Is Involved in the Resistance to the TP053 Antitubercular Prodrug. 10.3389/fmicb.2020.00292

New Insights into the Mechanism of Action of the Thienopyrimidine Antitubercular Prodrug TP053. 10.1021/acsinfecdis.9b00388

Vadim Makarov

Makarov Vadim / Vadim A. Makarov

ORCID: 0000-0001-8746-2694

https://publons.com/researcher/4233798/vadim-makarov/

Per aspera ad astra: Application of Simplex QSAR approach in antiviral research 10.4155/fmc.10.194

New pleconaril and [(biphenyloxy)propyl]isoxazole derivatives with substitutions in the central ring exhibit antiviral activity against pleconaril-resistant coxsackievirus B3 10.1016/j.antiviral.2008.09.002

Structure-based drug design and characterization of sulfonyl-piperazine benzothiazinone inhibitors of DprE1 from mycobacterium tuberculosis 10.1128/AAC.00681-18

The 8-pyrrole-benzothiazinones are noncovalent inhibitors of DprE1 from Mycobacterium tuberculosis 10.1128/AAC.00778-15

New 2-Ethylthio-4-methylaminoquinazoline derivatives inhibiting two subunits of cytochrome bc1 in Mycobacterium tuberculosis 10.1371/journal.ppat.1008270

Benzothiazinones: Prodrugs that covalently modify the decaprenylphosphoryl- β-D-ribose 2′-epimerase DprE1 of mycobacterium tuberculosis 10.1021/ja106357w

Identification of novel small-molecule histone deacetylase inhibitors by medium-throughput screening using a fluorigenic assay 10.1042/BJ20080536

Dispirotripiperazine-core compounds, their biological activity with a focus on broad antiviral property, and perspectives in drug design (mini-review) 10.1016/j.ejmech.2020.113014

Cmr is a redox-responsive regulator of DosR that contributes to M. tuberculosis virulence 10.1093/nar/gkx406

Binding of a N,N′-bisheteryl derivative of dispirotripiperazine to heparan sulfate residues on the cell surface specifically prevents infection of viruses from different families 10.1016/S0042-6822(03)00166-1

Benzothiazinones Kill Mycobacterium tuberculosis by blocking Arabinan synthesis 10.1126/science.1171583

Role of heparin and tissue type plasminogen activator in high altitude adaptation of the hemostasis system 10.1007/BF00840421

Synthesis of derivatives of a new heterocyclic system pyrazolo[3,4-b] pyrido[1′,2′: 1,2]imidazo[4,5-d]pyridine 10.1007/s11172-006-0322-z

Metabolic pathways of dithiocarbamates from laboratory powder diffraction data 10.1107/S0108270100013457

Synthesis of derivatives of pyrazolo[3,4-d]pyrimidines by reaction of 3,5-bis(dimethylaminomethylene)amino-4-methoxycarbonylpyrazole and 4-cyanopyrazole with amines 10.1023/A:1023780710982

Benzoylphenyl thiocyanates are new, effective inhibitors of the mycobacterial resuscitation promoting factor B protein 10.1186/s12941-017-0244-7

Development of macozinone for TB treatment: An update 10.3390/app10072269

Mechanism of resistance to an antitubercular 2-thiopyridine derivative that is also active against Burkholderia cenocepacia 10.1128/AAC.02438-13

Synthesis and NMR spectroscopic study of derivatives of pyrazolo[1,5-a]pyrimidines 10.1007/BF02291935

The effect of 2-thiocyanatopyridine derivative 11026103 on Burkholderia Cenocepacia: Resistance mechanisms and systemic impact 10.3390/antibiotics8040159

Novel [(biphenyloxy)propyl]isoxazole derivatives for inhibition of human rhinovirus 2 and coxsackievirus B3 replication 10.1093/jac/dki055

Specific Antiviral Activity of Pyrimidinedispirotripiperazinium Alone and in Combination with Acyclovir on a Herpes-Simplex-Virus Infection Model 10.1007/s11094-019-02079-9

4-dialkyldithiocarbamoyl-5-nitropyrimidines. Synthesis, structure, properties 10.1007/BF01184891

Highly polarized enamines. 3. Study of the spatial structure of α,α-diamino-β-cyano-β-nitroethylene derivatives 10.1007/BF02290751

Multiple Machine Learning Comparisons of HIV Cell-based and Reverse Transcriptase Data Sets 10.1021/acs.molpharmaceut.8b01297

Investigating the mechanism of action of diketopiperazines inhibitors of the burkholderia cenocepacia quorum sensing synthase CepI: A site-directed mutagenesis study 10.3389/fphar.2018.00836

Mycobacterium abscessus, an emerging and worrisome pathogen among cystic fibrosis patients 10.3390/ijms20235868

Discovery of prenylated flavonoids with dual activity against influenza virus and Streptococcus pneumoniae 10.1038/srep27156

Chemical, Metabolic, and Cellular Characterization of a FtsZ Inhibitor Effective Against Burkholderia cenocepacia 10.3389/fmicb.2020.00562

Rv2466c mediates the activation of TP053 to kill replicating and non-replicating Mycobacterium tuberculosis 10.1021/cb500149m

3,12-Diaza-6,9-diazoniadispiro[5.2.5.2]hexadecane dichloride from X-ray powder data 10.1107/S0108270199004138

The evolution of pleconaril: Modified o-alkyl linker analogs have biological activity towards coxsackievirus B3 Nancy 10.3390/molecules25061345

Study of the hemostatic properties of gaseous ozone 10.1007/BF02444668

Molecular determinants of inactivation of the resuscitation promoting factor B from Mycobacterium tuberculosis 10.1080/07391102.2012.698243

Synthesis, cytotoxicity and antiviral activity of N,N′-bis-5-nitropyrimidyl derivatives of dispirotripiperazine 10.1016/S0166-3542(02)00014-1

Molecular mechanism of a specific capsid binder resistance caused by mutations outside the binding pocket 10.1016/j.antiviral.2015.09.009

4-(N,N-Dialkylthiocarbamoylthio)-5-nitropyrimidines as new potential nitric oxide donors 10.1007/s11172-006-0203-5

New targets for HIV drug discovery 10.1016/j.drudis.2019.03.013

Mechanism of action of 5-nitrothiophenes against mycobacterium tuberculosis 10.1128/AAC.02693-13

Inhibition of transfer to secondary receptors by heparan sulfate-binding drug or antibody induces noninfectious uptake of human papillomavirus 10.1128/JVI.00998-07

In Vivo Activity of the Benzothiazinones PBTZ169 and BTZ043 against Nocardia brasiliensis 10.1371/journal.pntd.0004022

Biological and structural characterization of the Mycobacterium smegmatis nitroreductase NfnB, and its role in benzothiazinone resistance 10.1111/j.1365-2958.2010.07277.x

Study of antileprosy activities of some dialkyldithiocarbamate derivatives 10.1007/s10517-007-0111-1

Reactions of 4(6)-chloro-5-nitropyrimidines with nucleophilic agents (review) 10.1007/BF00810974

Synthesis and Some Biological Properties of Pyrrolo[1,2-a]indoles 10.1002/jhet.2312

3,5-Bis[(N,N-dimethylamino)methyleneamino]-1-methyl-4-nitropyrazole from X-ray powder diffraction data 10.1107/S010827010000860X

The cell division protein FtsZ as a cellular target to hit cystic fibrosis pathogens 10.1016/j.ejmech.2020.112132

Antileprosy activity and preliminary toxicological characteristics of some dialkyldithiocarbamate derivatives 10.1007/s10517-008-0114-6

Rv0579 Is Involved in the Resistance to the TP053 Antitubercular Prodrug 10.3389/fmicb.2020.00292

Design and Synthesis of Pyrano[3,2-b]indolones Showing Antimycobacterial Activity 10.1021/acsinfecdis.0c00622

Synthesis and properties of β,β-bisfunctionalised ketene N,N-acetals 10.1070/RC1998v067n11ABEH000422

Disturbance of antithrombogenic activity of the vessel wall in malignancy 10.1007/BF00791512

The past, present and future of RNA respiratory viruses: Influenza and coronaviruses 10.1093/femspd/ftaa046

How to kill dormant Mycobacterium tuberculosis 10.4103/ijmy.ijmy_106_18

Investigation of bisheteryl derivatives of piperazine and its analogs. 2. Synthesis and properties of bis(dialkyldithiocarbamoyl-5-nitro-4-pyrimidyl)piperazines 10.1007/BF01169676

WIN compounds: on the way to efficient antipicornaviral agent. A historical survey 10.1007/s11172-020-2811-x

Cryo-EM structure of pleconaril-resistant rhinovirus-B5 complexed to the antiviral OBR-5-340 reveals unexpected binding site 10.1073/pnas.1904732116

4,5-Diamino-1-phenyl-1,7-dihydro-6H-pyrazolo[3,4-b]pyridin-6-one in the synthesis of fused tricyclic systems 10.1007/s11172-007-0369-5

Intermolecular -CH3⋯O2N- contacts in two polymorphic modifications of (1E)-N′-[(E)-2-cyano-1-(dimethylamino)-2- nitrovinyl]-N,N-dimethylethanimidamide 10.1107/S0108768103010231

NOS2-deficient mice with hypoxic necrotizing lung lesions predict outcomes of tuberculosis chemotherapy in humans 10.1038/s41598-017-09177-2

QSAR analysis of [(biphenyloxy)propyl] isoxazoles: Agents against coxsackievirus B3 10.4155/fmc.10.278

Synthesis of pyrazolo [1,5-a] pyrimidines by the reaction of β-dicarbonyl compounds with 3,5-diamino-4-nitropyrazole 10.1007/BF02317814

Conversion of 4-chloro-5-nitropyrimidines to 1,3,5-triazines using alkylisothioureas 10.1007/BF00476222

Reaction of 3,5-diamino-4-nitropyrazole with electrophilic reagents 10.1007/BF02253106

Investigation of the reaction of 3,5-diamidino-4-nitropyrazole with amines 10.1023/A:1020921530209

Synthesis of Modified Peptides with C-Terminal α-Amino Aldehydes 10.1023/A:1011365401976

Transformations of ortho-methoxyaryl(hetaryl)carboxamides into quinazolin-4-one and pyrido[2,3-d]pyrimidin-4-one derivatives 10.1007/s11172-006-0057-x

Structural characterization of prazosin hydrochloride and prazosin free base 10.1002/jps.20204

Crystal and molecular structure of 1-amino-4-methoxycarbonyl-3-methyl-8-oxopyrazolo[1,5-a]pyrimidine monohydrate from laboratory powder data 10.1017/S0885715600010708

Copper-related toxicity in replicating and dormant Mycobacterium tuberculosis caused by 1-hydroxy-5-R-pyridine-2(1H)-thiones 10.1039/c8mt00067k

Discovery of new diketopiperazines inhibiting Burkholderia cenocepacia quorum sensing in vitro and in vivo 10.1038/srep32487

Competitive fitness of essential gene knockdowns reveals a broad-spectrum antibacterial inhibitor of the cell division protein FtsZ 10.1128/AAC.01231-18

Highly polarized enamines. 4. Unusual transformation of α,α-diamino-β-cyano-β-nitroethylene derivatives into 4,6-bisdimethylamino-5-nitropyrimidine 10.1007/BF02253108

Back to the future: Advances in development of broad-spectrum capsid-binding inhibitors of enteroviruses 10.1016/j.ejmech.2019.06.008

Anti-coxsackievirus B3 activity of 2-amino-3-nitropyrazolo[1,5-a] pyrimidines and their analogs 10.1016/j.bmcl.2004.10.043

Nitric oxide-releasing compounds for the treatment of lung infections 10.1016/j.drudis.2020.10.027

Amphiphilic star-shaped block copolymers as unimolecular drug delivery systems: Investigations using a novel fungicide 10.1039/c2sm26509e

Resuscitation-promoting Factors (Rpf): In Search of Inhibitors 10.2174/092986612802762723

A multitarget approach to drug discovery inhibiting Mycobacterium tuberculosis PyrG and PanK 10.1038/s41598-018-21614-4

A rapid method for estimation of the efficacy of potential antimicrobials in humans and animals by agar diffusion assay 10.1111/cbdd.13427

Synthesis and thermal transformations of 5-nitropyrimidin-4-yl dialkyldithiocarbamates 10.1023/B:RUCB.0000037858.17011.fb

The redox state regulates the conformation of Rv2466c to activate the antitubercular prodrug TP053 10.1074/jbc.M115.677039

Identification of individual structural fragments of N,N′-(bis-5-nitropyrimidyl)dispirotripiperazine derivatives for cytotoxicity and antiherpetic activity allows the prediction of new highly active compounds 10.1093/jac/dkm172

Study of the reaction of 3,5-diamino-4-carbomethoxypyrazole with acetoacetic ester. Synthesis of pyrazolo[1,5-a]pyrimidine 10.1007/BF02256848

Synthesis of pyrazolo[1,5-a]-pyrimidines by reaction of 3,5-diamino-4-nitropyrazole with acetoacetic ester in the presence of alkaline agents 10.1007/BF02256847

The antibacterial prodrug activator Rv2466c is a mycothiol-dependent reductase in the oxidative stress response of Mycobacterium tuberculosis 10.1074/jbc.M117.797837

Development and validation of a multiplex UHPLC-MS/MS method for the determination of the investigational antibiotic against multi-resistant tuberculosis macozinone (PBTZ169) and five active metabolites in human plasma 10.1371/journal.pone.0217139

Different influence of thrombolytic and physiological doses of single-chain urokinase-type plasminogen activator on washed platelets aggregation 10.1016/s0268-9499(96)80467-x

Finding of the low molecular weight inhibitors of resuscitation promoting factor enzymatic and resuscitation activity 10.1371/journal.pone.0008174

Crystal and molecular structures of 2-[1-(2-aminoethyl)-2-imidazolidinylidene]-2-nitroacetonitrile (C7H11N5O2) and 2,6-diamino-5-hydroxy-3-nitro-4H-pyrazolo[1,5-a]-pyrimidin-7-one monohydrate (C6H6N6O4·H2O) from X-ray, synchrotron and neutron powder diffraction data 10.1107/S010876819900213X

The in vivo environment accelerates generation of resuscitation-promoting factor-dependent mycobacteria 10.1164/rccm.201407-1289LE

Stable enhancement of tissue-type plasminogen activator levels in blood: Interrupted chamber hypoxia mimics effects of alpine hypoxia 10.1016/0268-9499(94)90254-2

New 1-hydroxy-2-thiopyridine derivatives active against both replicating and dormant Mycobacterium tuberculosis 10.1016/j.jiac.2017.04.012

Transformations of 5-nitropyrimidines 10.1002/jhet.5570450301

Susceptibility of coxsackievirus B3 laboratory strains and clinical isolates to the capsid function inhibitor pleconaril: Antiviral studies with virus chimeras demonstrate the crucial role of amino acid 1092 in treatment 10.1093/jac/dki263

DSTP-27 prevents entry of human cytomegalovirus 10.1128/AAC.01964-13

Optimized background regimen for treatment of active tuberculosis with the next-generation benzothiazinone macozinone (PBTZ169) 10.1128/AAC.00840-18

Towards a new combination therapy for tuberculosis with next generation benzothiazinones 10.1002/emmm.201303575

Quantitative structure-activity relationship studies of [(biphenyloxy)propyl]isoxazole derivatives. Inhibitors of human rhinovirus 2 replication 10.1021/jm0704806

Enamines as Synthons in the Synthesis of Heterocycles 10.1016/S0065-2725(08)60318-9

Clinical isolates of Mycobacterium tuberculosis in four European hospitals are uniformly susceptible to benzothiazinones 10.1128/AAC.01676-09

Synthesis and antileprosy activity of some dialkyldithiocarbamates 10.1093/jac/dkl095

6,11-Dioxobenzo[ f]pyrido[1,2- a]indoles Kill Mycobacterium tuberculosis by Targeting Iron-Sulfur Protein Rv0338c (IspQ), A Putative Redox Sensor 10.1021/acsinfecdis.0c00531

DprE1 - from the discovery to the promising tuberculosis drug target 10.2174/138161282027140630122724

Novel pleconaril derivatives: Influence of substituents in the isoxazole and phenyl rings on the antiviral activity against enteroviruses 10.1016/j.ejmech.2019.112007

Efflux-mediated resistance to a benzothiadiazol derivative effective against Burkholderia cenocepacia 10.3389/fmicb.2015.00815

New 2-Thiopyridines as potential candidates for killing both actively growing and dormant mycobacterium tuberculosis cells 10.1128/AAC.01308-13

Highly polarized enamines. 2. Synthesis and investigation of the further amination of derivatives of α,α-diamino-β-cyano-β-nitroethylene 10.1007/BF01164870

Fluorescent Benzothiazinone Analogues Efficiently and Selectively Label Dpre1 in Mycobacteria and Actinobacteria 10.1021/acschembio.8b00790

Highly polarized enamines 1. synthesis and some properties of β-tetrazolylenamines 10.1007/BF01169644

Investigation of bis-heteryl derivatives of piperazine and its analogs 1. Synthesis and conversions of n,n′-bis(2-r-5-nitro-6-pyrimidinyl)piperazines and n,n³-bis(2-r-5-nitro-6-pyrimidinyl)dispirotripiperazinium dichloride 10.1007/BF01169643

Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG 10.1016/j.chembiol.2015.05.016

Furoxanopyrimidines as exogenous donors of nitric oxide 10.1023/A:1022446208137

Antiretroviral activity of a novel pyrimidyl-di(Diazaspiroalkane) derivative 10.32607/20758251-2017-9-1-105-107

PEGylated mucus-penetrating nanocrystals for lung delivery of a new FtsZ inhibitor against Burkholderia cenocepacia infection 10.1016/j.nano.2019.102113

Molecule Property Analyses of Active Compounds for Mycobacterium tuberculosis 10.1021/acs.jmedchem.9b02075

Pyrazolopyrimidines: Potent Inhibitors Targeting the Capsid of Rhino- and Enteroviruses 10.1002/cmdc.201500304

Benzothiazinones are suicide inhibitors of mycobacterial decaprenylphosphoryl-β-d-ribofuranose 2′-oxidase DprE1 10.1021/ja211042r

New Insights into the Mechanism of Action of the Thienopyrimidine Antitubercular Prodrug TP053 10.1021/acsinfecdis.9b00388

2-carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1 10.1021/cb5007163

Synthesis of pyrazolo[3,4-b]pyridin-6-ones 10.1002/jhet.986

Pipeline of anti‐ Mycobacterium abscessus small molecules: Repurposable drugs and promising novel chemical entities 10.1002/med.21798

ALESSIO PORTA

PORTA ALESSIO

ORCID: 0000-0002-2564-9696

Fast low-pressurized microwave-assisted extraction of benzotriazole, benzothiazole and benezenesulfonamide compounds from soil samples 10.1016/j.talanta.2015.09.074

Competitive Gold-Promoted Meyer-Schuster and oxy-Cope Rearrangements of 3-Acyloxy-1,5-enynes: Selective Catalysis for the Synthesis of (+)-(S)-γ-Ionone and (-)-(2S,6 R)-cis-γ-Irone 10.1002/chem.201502382

Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG 10.1016/j.chembiol.2015.05.016

2-carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1 10.1021/cb5007163

Computational mechanistic study of the julia-kocieński reaction 10.1021/acs.joc.5b00008

General strategy for the synthesis of B1 and L1 prostanoids: Synthesis of phytoprostanes (RS)-9-L1-PhytoP, (R)-9-L1-PhytoP, (RS)-16-B1-PhytoP, and (RS)-16-L1-phytoP 10.1021/jo502538b

Enantioselective divergent synthesis of (-)-cis-α- and (-)-cis-γ-irone by using Wilkinson's catalyst 10.1002/chem.201404642

A unified stereodivergent strategy for prostaglandin and isoprostanoid synthesis 10.1021/jo500093k

First total synthesis of labeled EPA and DHA-derived A-type cyclopentenone isoprostanoids: [D2]-15-A3t-IsoP and [D 2]-17-A4t-NeuroP 10.1016/j.tet.2013.12.063

Structures and biological significance of lactarane sesquiterpenes from the European mushroom Russula nobilis 10.1016/j.phytochem.2014.08.018

A divergent enantioselective synthesis of 9-J1-phytoprostane and 9-A1-phytoprostane methyl ester 10.1002/ejoc.201301703

Biology and chemistry of neuroprostanes. First total synthesis of 17-A 4-NeuroP: Validation of a convergent strategy to a number of cyclopentenone neuroprostanes 10.1016/j.chemphyslip.2013.07.002

A concise and efficient total synthesis of oleocanthal 10.1002/ejoc.201300324

Stereodivergent strategy for neurofuran synthesis via palladium-catalyzed asymmetric allylic cyclization: Total synthesis of 7-epi-ST-Δ8- 10-neurofuran 10.1021/jo4004647

One-pot consecutive reactions based on the synthesis of conjugated enones by the re-catalysed meyer-schuster rearrangement 10.1002/chem.201201639

1H and 10B NMR and MRI investigation of boron- and gadolinium-boron compounds in boron neutron capture therapy 10.1016/j.apradiso.2011.02.021

The fatty acid oxidation product 15-A 3t-Isoprostane is a potent inhibitor of NFκB transcription and macrophage transformation 10.1111/j.1471-4159.2011.07422.x

Nuclear magnetic resonance study of Gd-based nanoparticles to tag boron compounds in boron neutron capture therapy 10.1063/1.3556951

Protecting group free synthesis of 6-substituted naphthols and binols 10.1021/jo1025892

Gold-mediated synthesis of α-ionone 10.1016/j.tetlet.2011.01.010

Improved synthesis of (E)-12-nitrooctadec-12-enoic acid, a potent PPARγ activator. development of a "buffer-Free" enzymatic method for hydrolysis of methyl esters 10.1021/jo101806m

The Meyer-Schuster rearrangement: A new synthetic strategy leading to prostaglandins and their drug analogs, Bimatoprost and Latanoprost 10.1016/j.tet.2010.07.069

Gold-catalyzed meyer-schuster rearrangement: Application to the synthesis of prostaglandins 10.1021/om1005534

Synthesis and assignment of absolute configuration of the Lridoid 9-deoxygelsemide 10.1021/ol902809v

Enantioselective synthesis and olfactory evaluation of bicyclic α- and γ-ionone derivatives: The 3D arrangement of key molecular features relevant to the violet odor of ionones 10.1021/jo9014936

A simple and versatile re-catalyzed meyer-schuster rearrangement of propargylic alcohols to α,β-unsaturated carbonyl compounds 10.1002/chem.200802622

Enantioselective synthesis and olfactory evaluation of 13-alkyl-substituted α-ionones 10.1002/cbdv.200890084

Electrophilic cyclopentenone neuroprostanes are anti-inflammatory mediators formed from the peroxidation of the ω-3 polyunsaturated fatty acid docosahexaenoic acid 10.1074/jbc.M803625200

Asymmetric synthesis of 14-A4t-neuroprostane: Hunting for a suitable biomarker for neurodegenerative diseases 10.1021/jo701719f

Antiinflammatory effects of the cyclopentenone isoprostane 15-A2-IsoP in human gestational tissues 10.1016/j.freeradbiomed.2007.03.009

Enantioselective synthesis of preclavulone A and its methyl ester 10.1016/j.tet.2007.03.003

Biomimetic cyclizations of functionalized isoprenoid polyenes: A cornucopia of synthetic opportunities 10.2174/138527206778742614

Asymmetric synthesis of a chiral building block for cyclopentanoids: A novel enantioselective synthesis of preclavulone A 10.1021/jo061321h

Identification of the major urinary metabolite of the highly reactive cyclopentenone isoprostane 15-A2t-isoprostane in vivo 10.1074/jbc.M502891200

A general enantioselective approach to jasmonoid fragrances: Synthesis of (+)-(1R,2S)-methyl dihydrojasmonate and (+)-(1R,2S)-magnolione 10.1021/jo050423p

The Cyclopentenone Product of Lipid Peroxidation, 15-A 2t-Isoprostane, Is Efficiently Metabolized by HepG2 Cells via Conjugation with Glutathione 10.1021/tx034213o

First enantioselective total synthesis of (8S,12R,15S)-prostaglandin J2 10.1021/jo034502h

First total synthesis of J2 isoprostane 10.1021/jo034658h

1,2-Oxopalladation versus π-allyl palladium route. A regioconvergent approach to a key intermediate for cyclopentanoids synthesis. New insights into the Pd(II)-catalyzed lactonization reaction 10.1021/jo025722i

First total synthesis of A2 isoprostane 10.1021/jo025652f

Laurent Roberto Chiarelli

Chiarelli Laurent Roberto

ORCID: 0000-0003-0348-9764

Tackling Critical Catalytic Residues in Helicobacter pylori L-Asparaginase 10.3390/biom5020306

Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG 10.1016/j.chembiol.2015.05.016

Engineering of helicobacter pylori lasparaginase: Characterization of two functionally distinct groups of mutants e0117025 10.1371/journal.pone.0117025

2-carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1 10.1021/cb5007163

Rv2466c mediates the activation of TP053 to kill replicating and non-replicating Mycobacterium tuberculosis 10.1021/cb500149m

Mechanism of action of 5-nitrothiophenes against mycobacterium tuberculosis 10.1128/AAC.02693-13

Biochemistry of lipolytic enzymes secreted by Penicillium solitum and Cladosporium cladosporioides 10.1080/09168451.2014.882752

4-Aminoquinolone piperidine amides: Noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity 10.1021/jm5005978

The DprE1 enzyme, one of the most vulnerable targets of Mycobacterium tuberculosis 10.1007/s00253-013-5218-x

Structural and energetic basis of protein kinetic destabilization in human phosphoglycerate kinase 1 deficiency 10.1021/bi301565m

Protein recognition by short peptide reversible inhibitors of the chromatin-modifying LSD1/CoREST lysine demethylase 10.1021/cb4001926

Monitoring of inosine monophosphate dehydrogenase activity and expression during the early period of mycophenolate mofetil therapy in de novo renal transplant patients 10.2133/dmpk.DMPK-12-RG-048

BEL -trefoil: A novel lectin with antineoplastic properties in king bolete (Boletus edulis) mushrooms 10.1093/glycob/cws164

Structural basis for benzothiazinone-mediated killing of Mycobacterium tuberculosis 10.1126/scitranslmed.3004395

Molecular insights on pathogenic effects of mutations causing phosphoglycerate kinase deficiency 10.1371/journal.pone.0032065

Letter to the Editor regarding Shibayama etal.: Biochemical and pathophysiological characterization of Helicobacter pylori asparaginase 10.1111/j.1348-0421.2012.00460.x

A new variant of phosphoglycerate kinase deficiency (p.I371K) with multiple tissue involvement: Molecular and functional characterization 10.1016/j.ymgme.2012.05.015

Structure of a lectin with antitumoral properties in king bolete (Boletus edulis) mushrooms 10.1093/glycob/cwr012

Analogous mechanisms of resistance to benzothiazinones and dinitrobenzamides in Mycobacterium smegmatis 10.1371/journal.pone.0026675

Mycobacterium tuberculosis phosphoribosylpyrophosphate synthetase: Biochemical features of a crucial enzyme for mycobacterial cell wall biosynthesis 10.1371/journal.pone.0015494

Inosine monophosphate dehydrogenase variability in renal transplant patients on long-term mycophenolate mofetil therapy 10.1111/j.1365-2125.2009.03542.x

Cell-cycle inhibition by Helicobacter pylori L-asparaginase 10.1371/journal.pone.0013892

Biological and structural characterization of the Mycobacterium smegmatis nitroreductase NfnB, and its role in benzothiazinone resistance 10.1111/j.1365-2958.2010.07277.x

Biochemical signatures of doppel protein in human astrocytomas to support prediction in tumor malignancy 10.1155/2010/301067

ThermoFAD, a Thermofluor^®-adapted flavin ad hoc detection system for protein folding and ligand binding 10.1111/j.1742-4658.2009.07006.x

Molecular basis of pyrimidine 5′-nucleotidase deficiency caused by 3 newly identified missense mutations (c.187T>C, c.469G>C and c.740T>C) and a tabulation of known mutations 10.1016/j.bcmd.2007.10.005

Helicobacter pylori l-asparaginase: A promising chemotherapeutic agent 10.1016/j.bbrc.2008.10.118

Pyruvate kinase deficiency: The genotype-phenotype association 10.1016/j.blre.2007.01.001

Erythrocyte adenylate kinase deficiency: characterization of recombinant mutant forms and relationship with nonspherocytic hemolytic anemia 10.1016/j.exphem.2007.05.004

Hereditary erythrocyte pyrimidine 5′-nucleotidase deficiency: A biochemical, genetic and clinical overview 10.1080/10245330500276667

Red cell pyruvate kinase deficiency: 17 New mutations of the PK-LR gene 10.1111/j.1365-2141.2005.05520.x

Functional analysis of pyrimidine 5′-nucleotidase mutants causing nonspherocytic hemolytic anemia 10.1182/blood-2004-10-3895

Pyrimidine 5′-nucleotidase activities detected in real samples by means of micellar electrokinetic chromatography 10.1002/elps.200406057

Structure and function of human erythrocyte pyruvate kinase: Molecular basis of nonspherocytic hemolytic anemia 10.1074/jbc.M202107200

Human erythrocyte pyruvate kinase: Characterization of the recombinant enzyme and a mutant form (R510Q) causing nonspherocytic hemolytic anemia 10.1182/blood.V98.10.3113

The allosteric regulation of pyruvate kinase: A site-directed mutagenesis study 10.1074/jbc.M001870200

Micellar electrokinetic chromatography as a complementary method to sodium dodecyl sulfate-polyacrylamide gel electrophoresis for studying limited proteolysis of proteins 10.1002/(SICI)1522-2683(19990801)20:12<2400::AID-ELPS2400>3.0.CO;2-T

The redox state regulates the conformation of Rv2466c to activate the antitubercular prodrug TP053 10.1074/jbc.M115.677039

Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043 10.1021/acsmedchemlett.5b00424

Micellar electrokinetic chromatography as a complementary method to sodium dodecyl sulfate-polyacrylamide gel electrophoresis for studying limited proteolysis of proteins 10.1002/(SICI)1522-2683(19990801)20:12<2400::AID-ELPS2400>3.0.CO;2-T

The Crystal Structure of Burkholderia cenocepacia DfsA Provides Insights into Substrate Recognition and Quorum Sensing Fatty Acid Biosynthesis 10.1021/acs.biochem.6b00178

Biochemical Characterization of Glutamate Racemase—A New Candidate Drug Target against Burkholderia cenocepacia Infections 10.1371/journal.pone.0167350

Iron acquisition pathways as targets for antitubercular drugs 10.2174/0929867323666160607223747

New and old hot drug targets in tuberculosis 10.2174/1389557516666160831164925

Discovery of new diketopiperazines inhibiting Burkholderia cenocepacia quorum sensing in vitro and in vivo 10.1038/srep32487

New prodrugs against tuberculosis 10.1016/j.drudis.2016.09.006

A Phenotypic Based Target Screening Approach Delivers New Antitubercular CTP Synthetase Inhibitors 10.1021/acsinfecdis.7b00006

Burkholderia cenocepacia infections in cystic fibrosis patients: Drug resistance and therapeutic approaches 10.3389/fmicb.2017.01592

Mechanochemical Synthesis and Biological Evaluation of Novel Isoniazid Derivatives with Potent Antitubercular Activity 10.3390/molecules22091457

A multitarget approach to drug discovery inhibiting Mycobacterium tuberculosis PyrG and PanK 10.1038/s41598-018-21614-4

Discovery and development of novel salicylate synthase (MbtI) furanic inhibitors as antitubercular agents 10.1016/j.ejmech.2018.06.033

New chromane-based derivatives as inhibitors of mycobacterium tuberculosis salicylate synthase (mbti): Preliminary biological evaluation and molecular modeling studies 10.3390/molecules23071506

Investigating the mechanism of action of diketopiperazines inhibitors of the burkholderia cenocepacia quorum sensing synthase CepI: A site-directed mutagenesis study 10.3389/fphar.2018.00836

Expanding Targets for a Metabolic Therapy of Cancer: L-Asparaginase 10.2174/97816080590891140301

The Role of One- and Two-Dimensional Electrophoretic Techniques in Proteomics of the Lung 10.5772/intechopen.75042

Erratum: Red cell pyruvate kinase deficiency: 17 New mutations of the PK-LR gene (British Journal of Haematology (2005) 129, (839-846)) 10.1111/j.1365-2141.2005.05691.x

Competitive fitness of essential gene knockdowns reveals a broad-spectrum antibacterial inhibitor of the cell division protein FtsZ 10.1128/AAC.01231-18

New insight into structure-activity of furan-based salicylate synthase (MbtI) inhibitors as potential antitubercular agents 10.1080/14756366.2019.1589462

Various Evolutionary Trajectories Lead to Loss of the Tobramycin-Potentiating Activity of the Quorum-Sensing Inhibitor Baicalin Hydrate in Burkholderia cenocepacia Biofilms 10.1128/AAC.02092-18

An overview on the potential antimycobacterial agents targeting serine/threonine protein kinases from Mycobacterium tuberculosis 10.2174/1568026619666190227182701

Quorum sensing as antivirulence target in cystic fibrosis pathogens 10.3390/ijms20081838

Phenylacetyl Coenzyme A, Not Phenylacetic Acid, Attenuates CepIR-Regulated Virulence in Burkholderia cenocepacia 10.1128/AEM.01594-19

PEGylated mucus-penetrating nanocrystals for lung delivery of a new FtsZ inhibitor against Burkholderia cenocepacia infection 10.1016/j.nano.2019.102113

New Insights into the Mechanism of Action of the Thienopyrimidine Antitubercular Prodrug TP053 10.1021/acsinfecdis.9b00388

Mycobacterium abscessus, an emerging and worrisome pathogen among cystic fibrosis patients 10.3390/ijms20235868

Promiscuous Targets for Antitubercular Drug Discovery: The Paradigm of DprE1 and MmpL3 10.3390/app10020623

Multitargeting Compounds: A Promising Strategy to Overcome Multi-Drug Resistant Tuberculosis 10.3390/molecules25051239

The cell division protein FtsZ as a cellular target to hit cystic fibrosis pathogens 10.1016/j.ejmech.2020.112132

Rv0579 Is Involved in the Resistance to the TP053 Antitubercular Prodrug 10.3389/fmicb.2020.00292

Antivirulence compounds: a future direction to overcome antibiotic resistance? 10.2217/fmb-2019-0294

6-Hydroxy-2-methylbenzofuran-4-carboxylic Acid 10.3390/M1143

Chemical, Metabolic, and Cellular Characterization of a FtsZ Inhibitor Effective Against Burkholderia cenocepacia 10.3389/fmicb.2020.00562

Shedding X-ray Light on the Role of Magnesium in the Activity of Mycobacterium tuberculosis Salicylate Synthase (MbtI) for Drug Design 10.1021/acs.jmedchem.0c00373

Editorial on Special Issue “Tuberculosis Drug Discovery and Development 2019” 10.3390/app10176069

Design, synthesis and evaluation of covalent inhibitors of DprE1 as antitubercular agents 10.1016/j.ejmech.2020.112773

Nitric oxide-releasing compounds for the treatment of lung infections 10.1016/j.drudis.2020.10.027

Synthesis, Characterization, and Biological Evaluation of New Derivatives Targeting MbtI as Antitubercular Agents 10.3390/ph14020155

A Coumarin-Based Analogue of Thiacetazone as Dual Covalent Inhibitor and Potential Fluorescent Label of HadA in Mycobacterium tuberculosis 10.1021/acsinfecdis.0c00325

Natural products against key Mycobacterium tuberculosis enzymatic targets: Emerging opportunities for drug discovery 10.1016/j.ejmech.2021.113732

The Antimalarial Mefloquine Shows Activity against Mycobacterium abscessus, Inhibiting Mycolic Acid Metabolism 10.3390/ijms22168533

Claudia Binda

Binda Claudia

ORCID: 0000-0003-2038-9845

www.unipv.it/biocry

An unprecedented NADPH domain conformation in lysine monooxygenase NbtG provides insights into uncoupling of oxygen consumption from substrate hydroxylation 10.1074/jbc.M114.629485

2-carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1 10.1021/cb5007163

Structure-based enzyme tailoring of 5-hydroxymethylfurfural oxidase 10.1021/acscatal.5b00031

4-Aminoquinolone piperidine amides: Noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity 10.1021/jm5005978

Kinetic and structural analysis of the irreversible inhibition of human monoamine oxidases by ASS234, a multi-target compound designed for use in Alzheimer's disease 10.1016/j.bbapap.2014.03.006

The DprE1 enzyme, one of the most vulnerable targets of Mycobacterium tuberculosis 10.1007/s00253-013-5218-x

Monoamine oxidase inhibitors: Diverse and surprising chemistry with expanding pharmacological potential 10.1007/978-94-007-6232-9-26

Structural basis for benzothiazinone-mediated killing of Mycobacterium tuberculosis 10.1126/scitranslmed.3004395

Molecular insights into human monoamine oxidase b inhibition by the glitazone antidiabetes drugs 10.1021/ml200196p

The 'gating' residues Ile199 and Tyr326 in human monoamine oxidase B function in substrate and inhibitor recognition 10.1111/j.1742-4658.2011.08386.x

Lights and shadows on monoamine oxidase inhibition in neuroprotective pharmacological therapies 10.2174/156802611798184355

Structural properties of human monoamine oxidases A and B 10.1016/B978-0-12-386467-3.00001-7

Interactions of monoamine oxidases with the antiepileptic drug zonisamide: Specificity of inhibition and structure of the human monoamine oxidase B complex 10.1021/jm101359c

Molecular mimicry and ligand recognition in binding and catalysis by the histone demethylase LSD1-CoREST complex 10.1016/j.str.2011.01.001

Potentiation of ligand binding through cooperative effects in monoamine oxidase B 10.1074/jbc.M110.169482

Biochemical, structural, and biological evaluation of tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and LSD2 10.1021/ja101557k

Alternative splicing of the histone demethylase LSD1/KDM1 contributes to the modulation of neurite morphogenesis in the mammalian nervous system 10.1523/JNEUROSCI.5500-09.2010

New roles of flavoproteins in molecular cell biology: Histone demethylase LSD1 and chromatin 10.1111/j.1742-4658.2009.07142.x

A novel mammalian flavin-dependent histone demethylase 10.1074/jbc.M109.003087

Molecular and mechanistic properties of the membrane-bound mitochondrial monoamine oxidases 10.1021/bi900413g

Structural and mechanistic studies of mofegiline inhibition of recombinant human monoamine oxidase B 10.1021/jm8011867

Structural and Mechanistic Studies of Arylalkylhydrazine Inhibition of Human Monoamine Oxidases a and B 10.1021/bi8002814

LSD1: oxidative chemistry for multifaceted functions in chromatin regulation 10.1016/j.tibs.2008.01.003

Structures of human monoamine oxidase B complexes with selective noncovalent inhibitors: Safinamide and coumarin analogs 10.1021/jm070677y

Structural insights into the mechanism of amine oxidation by monoamine oxidases A and B 10.1016/j.abb.2007.05.006

Structural basis of LSD1-CoREST selectivity in histone H3 recognition 10.1074/jbc.C700100200

New insights into the structures and functions of human monoamine oxidases A and B 10.1007/s00702-007-0674-z

8 Demethylation pathways for histone methyllysine residues 10.1016/S1874-6047(06)80010-7

A highly specific mechanism of histone H3-K4 recognition by histone demethylase LSD1 10.1074/jbc.M607411200

Functional role of the "aromatic cage" in human monoamine oxidase B: Structures and catalytic properties of Tyr435 mutant proteins 10.1021/bi051847g

Binding of rasagiline-related inhibitors to human monoamine oxidases: A kinetic and crystallographic analysis 10.1021/jm0506266

Human histone demethylase LSD1 reads the histone code 10.1074/jbc.M509549200

Three-dimensional structure of human monoamine oxidase A (MAO A): Relation to the structures of rat MAO A and human MAO B 10.1073/pnas.0505975102

Demonstration of isoleucine 199 as a structural determinant for the selective inhibition of human monoamine oxidase B by specific reversible inhibitors 10.1074/jbc.M500949200

Histone demethylation catalysed by LSD1 is a flavin-dependent oxidative process 10.1016/j.febslet.2005.03.015

Crystal structure of human monoamine oxidase B, a drug target enzyme monotopically inserted into the mitochondrial outer membrane 10.1016/S0014-5793(04)00209-1

Inactivation of Purified Human Recombinant Monoamine Oxidases A and B by Rasagiline and Its Analogues 10.1021/jm0310885

Crystal Structures of Monoamine Oxidase B in Complex with Four Inhibitors of the N-Propargylaminoindan Class 10.1021/jm031087c

The FAD Binding Sites of Human Monoamine Oxidases A and B 10.1016/S0161-813X(03)00114-1

Polystyrene microbridges used in sitting-drop crystallization release 1,4-diphenyl-2-butene, a novel inhibitor of human MAO B 10.1107/S0907444903016883

Insights into the mode of inhibition of human mitochondrial monoamine oxidase B from high-resolution crystal structures 10.1073/pnas.1633804100

Structure-function relationships in flavoenzyme-dependent amine oxidations: A comparison of polyamine oxidase and monoamine oxidase 10.1074/jbc.R200005200

Structure of human monoamine oxidase B, a drug target for the treatment of neurological disorders 10.1038/nsb732

Structural bases for inhibitor binding and catalysis in polyamine oxidase 10.1021/bi002751j

Cross-talk and ammonia channeling between active centers in the unexpected domain arrangement of glutamate synthase 10.1016/S0969-2126(00)00540-2

A 30 Å long U-shaped catalytic tunnel in the crystal structure of polyamine oxidase 10.1016/S0969-2126(99)80037-9

Crystallization and preliminary X-ray analysis of polyamine oxidase from Zea mays L. 10.1107/S0907444998005836

Tight-Binding Inhibition of Human Monoamine Oxidase B by Chromone Analogs: A Kinetic, Crystallographic, and Biological Analysis 10.1021/acs.jmedchem.8b00357

The structure of monoamine oxidases: past, present, and future 10.1007/s00702-018-1915-z

Structure-Based Engineering of Phanerochaete chrysosporium Alcohol Oxidase for Enhanced Oxidative Power toward Glycerol 10.1021/acs.biochem.8b00918

Crystallographic snapshots of UDP-glucuronic acid 4-epimerase ligand binding, rotation, and reduction 10.1074/jbc.RA120.014692

Promising Non-cytotoxic Monosubstituted Chalcones to Target Monoamine Oxidase-B 10.1021/acsmedchemlett.1c00238

Maria Rosalia PASCA

PASCA Maria Rosalia

ORCID: 0000-0002-8906-4937